2015年10月27日星期二

RS-127445|5-HT2B receptor antagonist|DC Chemicasl

RS-127445|5-HT2B receptor antagonist|DC Chemicasl

RS-127445 is a potent and selective antagonist at the serotonin 5-HT2B receptor, with around 1000x selectivity over the closely related 5-HT2A and 5-HT2C receptors.

Product Name: RS-127445 |Catalog Number:  DC8334 | cas: 199864-87-4 | Other names: RS-127445,RS 127445,RS127445,RS127,445,RS 127,445,RS-127,445 | Chemical name:4-(4-fluoro-1-naphthyl)-6-isopropylpyrimidin-2-amine | Molecule Formula: C17H16FN3.HCl | MW: 317.8

RS-127445 is a potent, selective and high affinity serotonin 5-HT2B receptor antagonist with a pIC50 of 10.4. The affinity (pKi) of RS-127445 for the 5-HT2B receptor is 9.5. RS-127445 is selective for the 5-HT2B receptor, having approximately 1000 fold selectivity over the human recombinant 5-HT2A, 5-HT2C, 5-HT5, 5-HT6 and 5-HT7 receptors, a 5-HT1A receptor in rat brain membranes, a 5-HT1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets. In the HEK-293 cells expressing the 5-HT2B receptor, RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pKB=9.5±0.1) and 5-HT-evoked increases in intracellular calcium (pIC50=10.4±0.1). In addition, RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus and (±) α-methyl-5-HT-mediated relaxation of the rat jugular vein with pA2 values of 9.5 and 9.9. In vivo, intraperitoneal administration of RS-127445 (5mg/kg) produces plasma concentrations predicted to fully saturate accessible 5-HT2B receptors for at least 4h. RS-127445 (0.1–10 µM) concentration-dependently reduces peristaltic frequency. RS-127445 (1–30 mg/kg), dose-dependently reduced faecal output, reaching significance at 10 and 30 mg/kg.

For research and scientific purpose only, not for human use.

SC-79,SC79|akt activator|DC Chemicals

SC-79,SC79|akt activator|DC Chemicals

SC-79 is an activator of Akt; binds to the pleckstrin homology domain of Akt.

Product Name: SC-79 |Catalog Number:  DC8333 | cas: 305834-79-1 | Other names: SC79,SC 79 | Chemical name:2-Amino-6-chloro-α-cyano-3-(ethoxycarbonyl)-4H-1-benzopyran-4-acetic acid ethyl ester | Molecule Formula: C17H17ClN2O5 | MW: 364.78

Activator of Akt; binds to the pleckstrin homology domain of Akt. Enhances Akt phosphorylation by upstream protein kinases; also enables cytosolic activation of Akt. Shown to suppress excitotoxicity-induced neuronal death in vitro and in vivo. Exhibits brain penetrance.

For research and scientific purpose only, not for human use.

GSK2256098|GSK-2256098|FAK inhibitor

GSK2256098|GSK-2256098|FAK inhibitor|DC Chemicals

GSK2256098 is  small molecule FAK kinase inhibitor.

Product Name: GSK2256098 |Catalog Number:  DC8331 | cas: N/A | Other names: GSK2256098,GSK-2256098,GSK 2256098 | Chemical name: 2-[(5-Chloro-2-{[3-methyl-1-(1-methylethyl)-1H-pyrazol-5-yl]amino}-4-pyridinyl)amino]-N-(methyloxy)benzamide; 2-[(5-chloro-2-{[3-methyl-1-(propan-2-yl)-1H-pyrazol-5-yl]amino}pyridin-4-yl)amino]-N-methoxybenzamide | Molecule Formula: C20H23ClN6O2 | MW: 414.88

GSK2256098 is  small molecule FAK kinase inhibitor.FAK inhibitor GSK2256098 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thereby inhibiting tumor cell migration, proliferation and survival, and tumor angiogenesis. The tyrosine kinase FAK is normally activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated and constitutively activated in various tumor cell types.

For research and scientific purpose only, not for human use.

NMS-P937 (NMS1286937)|cas 1034616-18-6|DC Chemicals

NMS-P937 (NMS1286937)|cas 1034616-18-6|DC Chemicals

NMS-P937 (NMS1286937) is an orally available, selective Polo-like Kinase 1 (PLK1) inhibitor with IC50 of 2 nM, 5000-fold selectivity over PLK2/PLK3. Phase 1.

Product Name: NMS-P937 (NMS1286937) |Catalog Number:  DC8445 | cas: 1034616-18-6 | Other names: NMS-P937,NMSP937,NMS P937 | Chemical name:4,5-dihydro-1-(2-hydroxyethyl)-8-[[5-(4-methyl-1-piperazinyl)-2-(trifluoromethoxy)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide | Molecule Formula: C24H27F3N8O3 | MW: 532.52

NMS-P937 shows a broad-spectrum antiproliferative activity against different solid tumor, leukemias and lymphomas cell lines. NMS-P937 potently causes a mitotic cell-cycle arrest followed by apoptosis in A2780 cells. [2]In mice xenografted with human HCT116 colon adenocarcinoma cells, NMS-P937 (90 mg/kg/d i.v. or p.o.) shows a significant tumor growth inhibition. [1] In mice bearing HT29, Colo205 colorectal, or A2780 ovarian xenograft tumors, NMS-P937 inhibits xenograft tumor growth. In addition, NMS-P937, in combination with approved cytotoxic drugs, causes enhanced tumor regression, and prolongs survival of animals.

For research and scientific purpose only, not for human use.


Sabutoclax|cas 1228108-65-3|DC Chemicals

Sabutoclax|cas 1228108-65-3|DC Chemicals

Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively..

Product Name: Sabutoclax |Catalog Number:  DC8444 | cas: 1228108-65-3 | Other names:  | Chemical name:[2,2'-Binaphthalene]-5,5'-dicarboxamide, 1,1',6,6',7,7'-hexahydroxy-3,3'-dimethyl-N5,N5'-bis[(2R)-2-phenylpropyl]-, (1R) | Molecule Formula: C42H40N2O8 | MW: 700.78

BI-97C1 potently inhibits cell growth of human prostate cancer, lung cancer, and lymphoma cell lines with EC50 values of 0.13, 0.56, and 0.049 μM, respectively, and shows little cytotoxicity against bax-/-bak-/- cells[1]. It is suggest that treatment with the combination regimen of mda-7/IL-24 and BI-97C1 induces autophagy that facilitates apoptosis in association with up-regulation of NOXA, accumulation of Bim, and activation of Bax and Bak[2].BI-97C1 displays in vivo efficacy in transgenic mice in which Bcl-2 is overexpressed in splenic B-cells and also demonstrates superior single-agent antitumor efficacy in a prostate cancer mouse xenograft model that depends on Mcl-1 for survival[1]. Treatment with Ad.5/3-mda-7 and BI-97C1 significantly inhibits the growth of human PC xenografts in nude mice and spontaneously induced PC in Hi-myc transgenic mice. Tumor growth inhibition correlats with increased TUNEL staining and decreased Ki-67 expression in both PC xenografts and prostates of Hi-myc mice

For research and scientific purpose only, not for human use.


ESI-09|cas 263707-16-0|DC Chemicals

ESI-09|cas 263707-16-0|DC Chemicals

ESI-09 is a specific exchange protein directly activated by cAMP (EPAC) inhibitor with IC50 of 3.2 μM and 1.4 μM for EPAC1 and EPAC2, respectively, >100-fold selectivity over PKA.

Product Name: ESI-09 |Catalog Number:  DC8443 | cas: 263707-16-0 | Other names: ESI-09,ESI 09,ESI09 | Chemical name:(E)-3-(5-tert-butylisoxazol-3-yl)-2-(2-(3-chlorophenyl)hydrazono)-3-oxopropanenitrile
 | Molecule Formula: C16H15ClN4O2 | MW: 330.77

ESI-09, a novel non-cyclic nucleotide EPAC antagonist, that is capable of specifically blocking intracellular EPAC-mediated Rap1 activation and Akt phosphorylation, as well as EPAC-mediated insulin secretion in pancreatic β cells. On the other hand, ESI-09 fails to suppress epidermal growth factor (EGF)-induced phosphorylation of Akt in AsPC1 cells. In pancreatic cancer cells, ESI-09 inhibits cells migration and invasion through decreasing 007-AM-induced cell adhesion dose-dependently. [1] ESI-09 significantly reduces intracellular and total bacterial counts in human umbilical vein endothelial cells. [2] ESI-09 effectively antagonizes Schwann cells (SC) differentiation induced by CPT-cAMP as well as the formation of myelin. In SC-neuron cultures, ESI-09 dramatically reduces the number of O1 positive and MBP positive SCs without compromising the health of the neurons or the SCs themselves. [3]ESI-09 (10 mg/kg/d, i.p.), via pharmacological inhibition of EPAC1, protects WT C57BL/6 mice from fatal SFG rickettsiosis.

For research and scientific purpose only, not for human use.

Nitenpyram|cas 150824-47-8|DC Chemicals

Nitenpyram|cas 150824-47-8|DC Chemicals

Product Name: Nitenpyram |Catalog Number:  DC8441 | cas: 150824-47-8 | Other names:  | Chemical name:(1E)-N-[(6-chloro-3-pyridinyl)methyl]-N-ethyl-N'-methyl-2-nitro-1,1-ethenediamine | Molecule Formula: C11H15ClN4O2 | MW: 270.72

For research and scientific purpose only, not for human use.

Erythromycin Cyclocarbonate|cas 55224-05-0|DC Chemicals

Erythromycin Cyclocarbonate|cas 55224-05-0|DC Chemicals

Erythromycin Cyclocarbonate, derivative of Erythromycin, inhibits protein synthesis of bacteria by binding to the 50S ribosome.

Product Name: Erythromycin Cyclocarbonate |Catalog Number:  DC8440 | cas: 55224-05-0 | Other names:  | Chemical name:cyclic 11,12-carbonate erythromycin | Molecule Formula: C38H65NO14 | MW: 759.92

For research and scientific purpose only, not for human use.

AGK2|cas 304896-28-4|DC Chemicals

AGK2|cas 304896-28-4|DC Chemicals

AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.

Product Name: AGK2 |Catalog Number:  DC8437 | cas: 304896-28-4 | Other names: AGK2,AGK-2,AGK 2 | Chemical name:2-cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-5-quinolinyl-2-propenamide | Molecule Formula: C23H13Cl2N3O2 | MW: 434.27

In SIRT2-myc-expressing HeLa cells, AGK2 effectively inhibits the activity of SIRT2, and increases acetylated tubulin. AGK2 protects dopaminergic neurons from α-Syn–induced toxicity in primary midbrain cultures. [1] AGK2 induces both necrosis and caspase-3-dependent apoptosis in C6 glioma cells. [2] SIRT2 also decreases merlin-mutant viability of mouse schwann cells (MSCs) without substantially reducing wild-type MSC viability. [3]In drosophila model of parkinson's disease, AGK2 rescues α-Syn–mediated toxicity and modify aggregation.

For research and scientific purpose only, not for human use.

Salmeterol Xinafoate|cas 94749-08-3|DC Chemicals

Salmeterol Xinafoate|cas 94749-08-3|DC Chemicals

Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.

Product Name: Salmeterol Xinafoate |Catalog Number:  DC8436 | cas: 94749-08-3 | Other names:  | Chemical name:4-hydroxy-α1-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol with 1-hydroxy-2-naphthalenecarboxylic acid(1:1) | Molecule Formula: C36H45NO7 | MW: 603.75

Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.

For research and scientific purpose only, not for human use.

LY2119620|cas 886047-22-9|DC Chemicals

LY2119620|cas 886047-22-9|DC Chemicals

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

Product Name: LY2119620 |Catalog Number:  DC8435 | cas: 886047-22-9 | Other names: LY2119620,LY-2119620,LY 2119620 | Chemical name:3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methyl-1-piperazinyl)-2-oxoethoxy]-thieno[2,3-b]pyridine-2-carboxamide | Molecule Formula: C19H24ClN5O3S | MW: 437.94

LY2119620 displays modest allosteric agonism and positively modulates the functional G protein–signaling ability of an agonist at the M2/M4 receptor subtypes by placing the M2 and M4 receptors into an active G protein–bound state. LY2119620 enhances the potency of three muscarinic acetylcholine receptor agonists, ACh, Oxo-M and iperoxo. [1] [3H]LY2119620 can be used as a probe for the human M(2) and M(4) muscarinic receptor allosteric binding sites.

For research and scientific purpose only, not for human use.

DTP3|cas N/A|DC Chemicals

DTP3|cas N/A|DC Chemicals

DTP3 is a selective GADD45β/MKK7 inhibitor, which inhibits cancer-selective NF-κB survival pathway.

Product Name: DTP3 |Catalog Number:  DC8430 | cas: N/A | Other names:  | Chemical name:(R)-2-((R)-2-acetamido-3-(4-hydroxyphenyl)propanamido)-N-((R)-1-amino-1-oxo-3-phenylpropan-2-yl)-5-guanidinopentanamide | Molecule Formula: C26H35N7O5 | MW: 525.6

DTP3 physically interacts with MKK7, both in isolation and within the complex with GADD45β, and dissociates the GADD45β/MKK7 complex via an allosteric mechanism. DTP3 selectively kills cells and induces apoptosis in MM cells with functional MKK7 and elevated GADD45β expression without toxicity to normal cells. In addition, DTP3 displays synergistic activity with bortezomib in two different MM cell lines, exhibiting a combination index of 0.21 in U266 cells and of 0.56 in KMS-12 cells. [1]DTP3 (14.5 mg/kg/day) exhibits potent antitumor activity against MM in mouse plasmacytoma model.

For research and scientific purpose only, not for human use.

Verdinexor (KPT-335)|cas 1392136-43-4|DC Chemicals

Verdinexor (KPT-335)|cas 1392136-43-4|DC Chemicals

Verdinexor (KPT-335) is an orally bioavailable, selective XPO1/CRM1 inhibitor.

Product Name: Verdinexor (KPT-335) |Catalog Number:  DC8429 | cas: 1392136-43-4 | Other names: KPT-335,KPT 335,KPT335 | Chemical name:(2Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]- 2-propenoic acid-2-(2-pyridinyl)hydrazide | Molecule Formula: C18H12F6N6O | MW: 442.32

Verdinexor inhibits the viability of Jurkat, OCI-Ly3, OCI-Ly10, and CLBL1 cells with IC50 of 0.3 nM, 2.1 nM, 41.8 nM, and 8.5 nM, respectively. KPT-335 also induces apoptosis in CLBL1 cells and primary canine DLBCL cells that express XPO1 and SINE. [1] Verdinexor potently and selectively inhibits vRNP export and effectively inhibits the replication of various influenza virus A and B strains, including pandemic H1N1 virus, highly pathogenic H5N1 avian influenza virus, and the recently emerged H7N9 strain. [2]Verdinexor (25 mg/kg twice daily, p.o.) reduces proinflammatory cytokine expression in the lung, produces in vivo antiviral activity by reducing lung virus titers, and thus reduces pulmonary disease pathogenesis and death associated with lethal influenza A virus challenge. [2] In autosomal-dominant polycystic kidney disease model, Verdinexor (5 mg/kg, i.p.) attenuates cyst growth via inhibition of XPO1.

For research and scientific purpose only, not for human use.

Lomitapide Mesylate|cas 202914-84-9|DC Chemicals

Lomitapide Mesylate|cas 202914-84-9|DC Chemicals

N-(2,2,2-trifluorethyl)-9-[4-[4-[[[4'-(trifluoromethyl)[1,1'-biphenyl]-2-yl]carbonyl]amino]-1-piperidinyl]butyl]-9H-fluorene-9-carboxamide methanesulfonate

Product Name: Lomitapide Mesylate |Catalog Number:  DC8428 | cas: 202914-84-9 | Other names:  | Chemical name: | Molecule Formula: C40H41F6N3O5S  | MW: 789.83

For research and scientific purpose only, not for human use.

Isepamicin Sulphate|cas 67814-76-0|DC Chemicals

Isepamicin Sulphate|cas 67814-76-0|DC Chemicals

Isepamicin Sulphate is an aminoglycoside antibiotic, which inhibits bacterial protein synthesis by targeting the bacterial 30S ribosomal subunit.

Product Name: Isepamicin Sulphate |Catalog Number:  DC8427 | cas: 67814-76-0 | Other names:  | Chemical name:O-6-amino-6-deoxy-α-D-glucopyranosyl-(1→4)-O-[3-deoxy-4-C-methyl-3-(methylamino)-β-L-arabinopyranosyl-(1→6)]-N1-[(3S)-3-amino-2-hydroxy-1-oxopropyl]-2-deoxy-D-strepta | Molecule Formula: C22H45N5O16S | MW: 667.68

For research and scientific purpose only, not for human use.

Picropodophyllin (PPP)|cas 477-47-4|DC Chemicals

Picropodophyllin (PPP)|cas 477-47-4|DC Chemicals

Picropodophyllin (PPP) is a selective IGF-1R inhibitor with IC50 of 1 nM. Phase 1/2.

Product Name: Picropodophyllin (PPP) |Catalog Number:  DC8426 | cas: 477-47-4 | Other names:  | Chemical name:(5R,5aS,8aR,9R)-5,8,8a,9-tetrahydro-9-hydroxy-5-(3,4,5-trimethoxyphenyl)-furo[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one | Molecule Formula: C22H22O8 | MW: 414.41

In intact cells, PPP efficiently inhibits IGF-1-stimulated IGF-1R, Akt (Ser 473) and Erk1/2 phosphorylation. Picropodophyllin specifically inhibits cell growth, and induces apoptosis in cultured IGF-1R-positive tumor cells. [1] Picropodophyllin synergistically sensitizes HMCL, primary human MM and murine 5T33MM cells to ABT-737 and ABT-199 by further decreasing cell viability and enhancing apoptosis. [3] Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells. [4]In SCID mice xenografted with human ES-1, BE, and PC3, Picropodophyllin (20 mg/kg/12 h, i.p.) causes complete tumor regression. [1] In the 5T33MM mouse model, Picropodophyllin also shows a marked antitumor activity, and causes a significant increase in survival.

For research and scientific purpose only, not for human use.

SecinH3|cas 853625-60-2|DC Chemicals

SecinH3|cas 853625-60-2|DC Chemicals

SecinH3 is a selective cytohesin inhibitor with IC50 of 2.4 μM, 5.4 μM, 5.4 μM, 5.6 μM, 5.6 μM, and 65 μM for hCyh2, hCyh1, mCyh3, hCyh3, drosophila steppke, and yGea2-S7, respectively.

Product Name: SecinH3 |Catalog Number:  DC8424 | cas: 853625-60-2 | Other names:  | Chemical name:N-(4-(5-(benzo[d][1,3]dioxol-5-yl)-3-methoxy-1H-1,2,4-triazol-1-yl)phenyl)-2-(phenylthio)acetamide | Molecule Formula: C24H20N4O4S | MW: 460.5

In HepG2 cells, SecinH3 inhibits insulin signaling and associated gene expression. [1] SecinH3 also markedly inhibits migration of preadipocyte 3T3-L1 cells. [2] In the A549 cells, SecinH3 results in reduced proliferation by indirectly attenuating EGFR activation, and causes a synergistic antiproliferative effect when used in combination with gefitinib. [3]In mice, SecinH3 increases the expression of gluconeogenic genes, reduces the expression of glycolytic, fatty acid and ketone body metabolism genes in the liver, reduces liver glycogen stores, and increases plasma insulin. [1] In mice bearing H460 xenografts, SecinH3 significantly retards tumor growth through its antiproliferative and pro-apoptotic effect.

For research and scientific purpose only, not for human use.

4SC-202|cas 910462-43-0|DC Chemicals

4SC-202|cas 910462-43-0|DC Chemicals

4SC-202 is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.

Product Name: 4SC-202 |Catalog Number:  DC8423 | cas: 910462-43-0 | Other names: 4SC-202,4SC 202,4SC202 | Chemical name:(E)-N-(2-aminophenyl)-3-(1-(4-(1-methyl-1H-pyrazol-4-yl)phenylsulfonyl)-1H-pyrrol-3-yl)acrylamide | Molecule Formula: C23H21N5O3S | MW: 447.51

In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. [1]In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model.

For research and scientific purpose only, not for human use.

GSK2830371|cas 1404456-53-6|DC Chemicals

GSK2830371|cas 1404456-53-6|DC Chemicals

GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.

Product Name: GSK2830371 |Catalog Number:  DC8422 | cas: 1404456-53-6 | Other names: GSK2830371,GSK 2830371,GSK-2830371 | Chemical name:(S)-5-((5-chloro-2-methylpyridin-3-ylamino)methyl)-N-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide | Molecule Formula: C23H29ClN4O2S | MW: 461.02

In the PPM1D-amplified MCF7 breast carcinoma cells, GSK2830371 increases the phosphorylation of multiple Wip1 substrates, including p53 (S15), Chk2 (T68), H2AX (S139) and ATM (S1981). GSK2830371 shows selective antiproliferative activity in a subset of lymphoid cell lines, all of which carry a wild-type TP53 allele. Furthermore, co-treatment of doxorubicin and GSK2830371 results in a synergistic antiproliferative effect in DOHH2 and MX-1 tumor cells. [1]In vivo, GSK2830371 increases phosphorylation of Chk2 (T68) and p53 (S15) and decreases Wip1 protein concentrations in DOHH2 tumors. GSK2830371 (150 mg/kg p.o.) also inhibits the growth of DOHH2 tumor xenografts via inhibition of Wip1.

For research and scientific purpose only, not for human use.

FTI 277 HCl|cas 180977-34-8|DC Chemicals

FTI 277 HCl|cas 180977-34-8|DC Chemicals

FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I.

Product Name: FTI 277 HCl |Catalog Number:  DC8421 | cas: 180977-34-8 | Other names: FTI277,FTI-277,FTI 277 | Chemical name:4-[2(R)-amino-3-mercaptopropyl]amino-2-phenylbenzoyl-(S)-methionine methyl ester hydrochloride | Molecule Formula: C22H30ClN3O3S2 | MW: 484.07

FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 induces accumulation of cytoplasmic non-farnesylated H-Ras, accumulates inactive Ras/Raf complexes in the cytoplasm, and blocks constitutive MAPK activation in H-RasF cells. [1] FTI-277 causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. [2] FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. [3] In SH-SY5Y cells, FTI-277 diminishes the toxic effects of methamphetamine on induction in cell degeneration, activation in c-Jun-N-terminal kinase cascades, and Ras activation. [4]In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia.

For research and scientific purpose only, not for human use.

Salirasib|cas 162520-00-5|DC Chemicals

Salirasib|cas 162520-00-5|DC Chemicals

Salirasib is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Phase 2.

Product Name: Salirasib |Catalog Number:  DC8420 | cas: 162520-00-5 | Other names: Salirasib | Chemical name:2-((2E,6E)-3,7,11-trimethyldodeca-2,6,10-trienylthio)benzoic acid | Molecule Formula: C22H30O2S | MW: 358.54

Salirasib inhibits the growth of human Ha-ras-transformed Rat1 cells, which correlates well with their inhibition for PPMTase. [1] Salirasib inhibits Ras methylation in Rat-1 fibroblasts, Ras-transformed Rat-1, and B16 melanoma cells. Salirasib also reduces the levels of Ras in cell membranes and inhibits Ras-dependent cell growth, independently of methylation, but via modulation of Ras-Raf communication. [2] In Ras-transformed EJ cells, Salirasib interferes with the activation of Raf-1 and MAPK and inhibits DNA synthesis. [3]In Panc-1 xenografted nude mice, Salirasib (5 mg/kg i.p.) markedly inhibits tumor growth without systemic toxicity. [4] In male Wistar rats, Salirasib (5 mg/kg i.p.) markedly inhibits thioacetamide-induced -induced liver cirrhosis. [5] In the dy(2J)/dy(2J) mouse model of congenital muscular dystrophy, Salirasib (5 mg/kg i.p.) attenuates fibrosis and improves muscle strength.

For research and scientific purpose only, not for human use.

SB-334867|cas 792173-99-0|DC Chemicals

SB-334867|cas 792173-99-0|DC Chemicals

SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

Product Name: SB-334867 |Catalog Number:  DC8419 | cas: 792173-99-0 | Other names: SB334867,SB 334867,SB-334867 | Chemical name:1-(2-methylbenzo[d]oxazol-6-yl)-3-(1,5-naphthyridin-4-yl)urea | Molecule Formula: C17H13N5O2 | MW: 319.32

In CHO-OX1 cells, SB-334867 inhibits the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses with pKB of 7.27 and 7.23 respectively, without effect on the UTP (3 microM)-induced calcium response. [1]In both male and female rats, SB-334867 (30 mg/kg, i.p.) significantly reduces natural and orexin-A-induced food intake. [2] SB-334867 (2 mg/kg, i.v.) blocks the effects of antipsychotic drugs on dopamine neuronal activity in rats. [3] SB-334867 also inhibits the development of morphine analgesic tolerance in rats.

For research and scientific purpose only, not for human use.

CH5183284 (Debio-1347)|cas 1265229-25-1|DC Chemicals

CH5183284 (Debio-1347)|cas 1265229-25-1|DC Chemicals

CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.

Product Name: CH5183284 (Debio-1347) |Catalog Number:  DC8418 | cas: 1265229-25-1 | Other names: CH5183284,CH-5183284,CH 5183284 | Chemical name:(5-amino-1-(2-methyl-3H-benzo[d]imidazol-5-yl)-1H-pyrazol-4-yl)(1H-indol-2-yl)methanone | Molecule Formula: C20H16N6O | MW: 356.38

In cell-based assay, CH5183284 prevents autophosphorylation of FGFR1, FGFR2, and FGFR3 at 100 to 300 nM in the DMS114 (FGFR1 amplification), SNU-16 (FGFR2 amplification), and KMS11 [t(4;14) translocation and FGFR3 Y373C mutation] cell lines. CH5183284 thus produces selective antiproliferative activity against cancer cell lines harboring genetic alterations in FGFR. CH5183284 also inhibit FGFR2 harboring one type of the gatekeeper mutation (V564F) that causes resistance to other FGFR inhibitors. [1]CH5183284 (100 mg/kg/day, p.o.) shows selective and significant antitumor activity against xenografts with FGFR genetic alterations such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), SNU-16 (gastric cancer, FGFR2 amplification), MFE-280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion).

For research and scientific purpose only, not for human use.

SB273005|cas 205678-31-5|DC Chemicals

SB273005|cas 205678-31-5|DC Chemicals

SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.

Product Name: SB273005 |Catalog Number:  DC8417 | cas: 205678-31-5 | Other names: SB 273005,SB-273005,SB273005 | Chemical name:(S)-2-(8-(2-(6-(methylamino)pyridin-2-yl)ethoxy)-3-oxo-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-benzo[c]azepin-4-yl)acetic acid | Molecule Formula: C22H24F3N3O4 | MW: 451.44

In vitro, SB273005 inhibits human osteoclast-mediated bone resorption with IC50 of 11 nM. [1] In blood containing MDA-MB-231 cells, a combination of SB273005 and lamifiban inhibits tumor cell adhesion to vascular extracellular matrix (ECM). [3]In rat models of bone resorption and osteoporosis, SB273005 (30 mg/kg, p.o.) inhibits the parathyroid hormone-stimulated calcemic response, and inhibits bone loss. [1] In rat with adjuvant-induced arthritis, SB273005 (60 mg/kg, p.o.) significantly reduces the symptoms of adjuvant-induced arthritis. [2] SB273005 (1000 mg/kg/day, p.o.) causes acute, transient necrosis of vascular smooth muscle cell (VSMC) in aorta and renal arteries of mice. [4] In pregnant mice, SB273005 reverses the reduction of Th1 cell-produced IL-2 levels and the increase of Th2 cell-derived IL-10 levels.

For research and scientific purpose only, not for human use.

MI-773 (SAR405838)|cas 1303607-60-4|DC Chemicals

MI-773 (SAR405838)|cas 1303607-60-4|DC Chemicals

MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

Product Name: MI-773 (SAR405838) |Catalog Number:  DC8414 | cas: 1303607-60-4 | Other names: SAR405838,SAR-405838,SAR 405838 | Chemical name:(2'S,3R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-N-(trans-4-hydroxycyclohexyl)-2-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide | Molecule Formula: C29H34Cl2FN3O3 | MW: 562.5

MI-773 binds to MDM2 with Ki of 0.88 nM. MI-773 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells. [1]In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,).

For research and scientific purpose only, not for human use.

STF-083010|cas 307543-71-1|DC Chemicals

STF-083010|cas 307543-71-1|DC Chemicals

STF-083010 is a specific IRE1α endonuclease inhibitor.

Product Name: STF-083010 |Catalog Number:  DC8413 | cas: 307543-71-1 | Other names: STF-083010,STF083010,STF 083010 | Chemical name:(E)-N-((2-hydroxynaphthalen-1-yl)methylene)thiophene-2-sulfonamide | Molecule Formula: C15H11NO3S2 | MW: 317.38

In RPMI 8226, MM.1S, and MM.1R MM cell lines, STF-083010 exhibits cytostatic and cytotoxic activity in a dose and time dependent manner. [1] [2] In MiaPaCa2, Panc0403, and SU8686 cell lines, STF-083010 inhibits XBP1 splicing and blocks IRE1α's endonuclease activity without affecting its kinase activity. [1] In Eμ-TCL1 CLL cells, STF-083010 exhibits about 70% growth inhibition after 3 days culture. In MEC1 and MEC2 cells, STF-083010 produces 20% growth inhibition in 48 h. WaC3 cells respond to treatments with STF-083010 with gradually decreased growth. [3]In human multiple myeloma (MM) xenografts model, STF-083010 (i.p., 30 mg/kg) significantly inhibits the growth of tumor.

For research and scientific purpose only, not for human use.

SRT2104 (GSK2245840)|cas 1093403-33-8|DC Chemicals

SRT2104 (GSK2245840)|cas 1093403-33-8|DC Chemicals

SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.

Product Name: SRT2104 (GSK2245840) |Catalog Number:  DC8412 | cas: 1093403-33-8 | Other names: GSK 2245840,GSK-2245840,GSK2245840,SRT-2104,SRT 2104 | Chemical name:4-methyl-N-(2-(3-(morpholinomethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-(pyridin-3-yl)thiazole-5-carboxamide | Molecule Formula: C26H24N6O2S2 | MW: 516.64

SRT2104 reduces p65/RelA acetylation levels in C2C12 cells.[1]In male C57BL/6J mice, SRT2104 (100 mg/kg, p.o.) extends both mean and maximal lifespan of mice fed a standard diet, and enhances motor coordination, bone mineral density, and insulin sensitivity and decreased inflammation. Short-term SRT2104 treatment preserves bone and muscle mass in an experimental model of atrophy.[1] In Male N171-82Q HD mice, SRT2104 (diet containing 0.5% SRT2104) effectively penetrates the blood-brain barrier, attenuates brain atrophy, improves motor function, and extends survival.

For research and scientific purpose only, not for human use.

Afuresertib (GSK2110183)|cas 1047644-62-1|DC Chemicals

Afuresertib (GSK2110183)|cas 1047644-62-1|DC Chemicals

Afuresertib (GSK2110183) is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Product Name: Afuresertib (GSK2110183)
 |Catalog Number:  DC8411 | cas: 1047644-62-1 | Other names:  | Chemical name:N-((S)-1-amino-3-(3-fluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)thiophene-2-carboxamide | Molecule Formula: C18H17Cl2FN4OS | MW: 427.32

Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib.[1]Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively.

For research and scientific purpose only, not for human use.

GNE-317|cas 1394076-92-6|DC Chemicals

GNE-317|cas 1394076-92-6|DC Chemicals

GNE-317 is a potent, brain-penetrant PI3K inhibitor.

Product Name: GNE-317 |Catalog Number:  DC8410 | cas: 1394076-92-6 | Other names: GNE-317,GNE 317,GNE317 | Chemical name:5-(6-(3-methoxyoxetan-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine | Molecule Formula: C19H22N6O3S | MW: 414.48

GNE-317 is not a substrate of P-gp or BCRP transporter in transfected Madin-Darby canine kidney (MDCK) cells. Binding of GNE-317 to plasma proteins exhibits a free fraction of 14.9 % in mouse plasma, and binding to brain tissues is higher, with a free fraction of 5.4%. GNE-317 shows cytostasis but no cell death to U87 cells.[1]GNE-317 (40 mg/kg, p.o.) markedly inhibits the PI3K pathway in mouse brain, causing 40% to 90% suppression of the pAkt and pS6 signals up to 6-hour postdose. GNE-317 (40 mg/kg, p.o.) is efficacious in the U87 and GS2 orthotopic models, achieving tumor growth inhibition of 90% and 50%, respectively. In the GBM10 tumor model, GNE-317 (30 mg/kg, p.o.; 40 mg/kg the first 2 weeks) extends the survival of mice from a median of 55.5 to 75 days.

For research and scientific purpose only, not for human use.

BRD7552|cas 1137359-47-7|DC Chemicals

BRD7552|cas 1137359-47-7|DC Chemicals

BRD7552 is an inducer of transcription factor PDX1, which increases insulin expression.

Product Name: BRD7552 |Catalog Number:  DC8409 | cas: 1137359-47-7 | Other names: BRD 7552,BRD-7552,BRD7552 | Chemical name:ethyl 4-(((2R,3R,4S,5R,6S)-4,5-bis(benzo[d][1,3]dioxol-5-ylcarbamoyloxy)-2-(hydroxymethyl)-6-methoxy-tetrahydro-2H-pyran-3-yloxy)carbonyl)benzoate | Molecule Formula: C33H33N3O15 | MW: 711.63

BRD7552 upregulates PDX1 expression in both primary human islets and ductal cells, and induces epigenetic changes in the PDX1 promoter consistent with transcriptional activation. BRD7552 increases PDX1 mRNA levels by 2- to 4-fold, with a maximal effect at 5 μM and the expression of MAFA. BRD7552 increases PDX1 expression in mouse αTC cells but not βTC cells. Treatment of PANC-1 cells with BRD7552 causes a dose-dependent increase in insulin mRNA expression.

For research and scientific purpose only, not for human use.

Naloxone HCl Dihydrate|cas 51481-60-8|DC Chemicals

Naloxone HCl Dihydrate|cas 51481-60-8|DC Chemicals

Naloxone HCl Dihydrate is an opioid inverse agonist drug used to counter the effects of opiate overdose.

Product Name: Naloxone HCl Dihydrate |Catalog Number:  DC8407 | cas: 51481-60-8 | Other names:  | Chemical name:naloxone hydrochloride dihydrate | Molecule Formula: C19H26ClNO6 | MW: 399.87

The Ki values of (−)-naloxone for the MOR, KOR, and DOR are 0.559 nM, 4.91 nM, and 36.5 nM, respectively. Naloxone HCl Dihydrate binds to the MOR with approximately 9-fold greater affinity relative to the KOR and around 60-fold greater affinity relative to the DOR.[1]The combination of Naloxone HCl Dihydrate (0.5 mg/kg, i.p.) with tramadol (22 mg/kg) decreases the antiallodynic effect of tramadol.

For research and scientific purpose only, not for human use.

2015年10月26日星期一

A-438079 HCl|cas 899431-18-6|DC Chemicals

A-438079 HCl|cas 899431-18-6|DC Chemicals

A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

Product Name: A-438079 HCl |Catalog Number:  DC8406 | cas: 899431-18-6 | Other names: A-438079,A438079,A 438079 | Chemical name:3-((5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl)methyl)pyridine hydrochloride | Molecule Formula: C13H10Cl3N5 | MW: 342.61

In 1321N1 cells stably expressing rat P2X7 receptors, A-438079 blocks BzATP-(10 μM) evoked changes in intracellular calcium concentrations with an IC50 of 321 nM. A-438079 is also selective for the P2X7 receptor, at concentrations up to 100 μM.[1]Intraperitoneal injection of A-438079 (5 and 15 mg/kg) 60 min after triggering seizures reduces seizure severity and neuronal death within the hippocampus. A-438079 has superior neuroprotective effects compared with an equally dose of phenobarbital (25 mg/kg).[2] A-438079 partially but significantly prevents the 6-OHDA-induced depletion of striatal DA stores.[3] Pretreatment with A-438079 reduces nociceptive behaviour scores in the HC model.[4] A-438079 (80 μmol/kg, i.v.) reduces noxious and innocuous evoked activity of different classes of spinal neurons in neuropathic rats. A-438079 (100 and 300 μmol/kg, i.p.) significantly raises withdrawal thresh-olds in both the SNL and CCI models.

For research and scientific purpose only, not for human use.

E3330|cas 136164-66-4|DC Chemicals

E3330|cas 136164-66-4|DC Chemicals

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

Product Name: E3330 |Catalog Number:  DC8404 | cas: 136164-66-4 | Other names:  | Chemical name:(2E)-2-[(4,5-dimethoxy-2-methyl-3,6-dioxo-1,4-cyclohexadien-1-yl)methylene]-undecanoic acid | Molecule Formula: C21H30O6 | MW: 378.46

 E3330 affects hemangioblast development in vitro via inhibition of Ape1 redox activity. [1] E3330 inhibits the growth of human pancreatic cancer cell line PANC1, XPA1, MIAPACA, BxPC3, and PK9. E3330 also promotes exit of cell cycle in PANC1 cells, inhibits the DNA-Binding activity of HIF-1α and migration of pancreatic cancer cells. [2] In JHH6 cells, E3330 prevents the functional activation of NF-κB via the alteration of APE1 subcellular trafficking and reduces IL-6 and IL-8 expression induced by TNF-α and FAs accumulation through blockage of the redox-mediated activation of NF-κB. [3]In mice with endotoxin-mediated hepatitis, E3330 (300 mg/kg, p.o.) attenuates the elevation of plasma tumor necrosis factor activity and protectes mice from liver injury. [4] In Rat model, E3330 (100 mg/kg, p.o.) also protectes rats from severe liver injury induced with endotoxin plus galactosamine.

For research and scientific purpose only, not for human use.

Endoxifen HCl|cas 1032008-74-4|DC Chemicals

Endoxifen HCl|cas 1032008-74-4|DC Chemicals

Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

Product Name: Endoxifen HCl |Catalog Number:  DC8403 | cas: 1032008-74-4 | Other names:  | Chemical name:4-[(1Z)-1-[4-[2-(methylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-phenol, hydrochloride (1:1) | Molecule Formula: C25H28ClNO2 | MW: 409.95

Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. [1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. [2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. [3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. [4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. [5]In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen.

For research and scientific purpose only, not for human use.

BI-847325|cas 1207293-36-4|DC Chemicals

BI-847325|cas 1207293-36-4|DC Chemicals

BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

Product Name: BI-847325 |Catalog Number:  DC8401 | cas: 1207293-36-4 | Other names: BI-847325,BI 847325,BI847325 | Chemical name:(Z)-3-(3-((4-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-2-oxoindolin-6-yl)-N-ethylpropiolamide | Molecule Formula: C29H28N4O2 | MW: 464.56

BI-847325 shows growth-inhibitory effects on BRAF-mutant and vemurafenib-resistant melanoma cells with IC50 ranging from 0.3 nM to 2 μM, and prevents colony formation in six BRAF-mutant melanoma cell lines. BI-847325 also induces apoptosis by reducing Mcl-1 expression. [1]In mice bearing 1205Lu and 1205LuR xenografts, BI-847325 (75 mg/kg, p.o.) causes significant tumor suppression without significant alteration in the body weights.

For research and scientific purpose only, not for human use.

AZD3839|cas 1227163-84-9|DC Chemicals

AZD3839|cas 1227163-84-9|DC Chemicals

AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

Product Name: AZD3839 |Catalog Number:  DC8400 | cas: 1227163-84-9 | Other names: AZD3839,AZD-3839,AZD 3839 | Chemical name:(S)-3-(2-(difluoromethyl)pyridin-4-yl)-7-fluoro-3-(3-(pyrimidin-5-yl)phenyl)-3H-isoindol-1-amine | Molecule Formula: C24H16F3N5 | MW: 431.41

In SH-SY5Y cells, AZD3839 efficiently decreases the Aβ40 levels with IC50 of 4.8 nM, and decreases the formation of sAPPβ with IC50 of 16.7 nM. AZD3839 also decreases the Aβ40 levels secreted from C57BL/6 mouse primary cortical neurons, N2A cells, and Dunkin-Hartley guinea pig primary cortical neurons with IC50 values of 50.9, 32.2, and 24.8 nM, respectively. [1] AZD3839 causes in vitro BACE1 inhibition in the cell assay with IC50 value of 16.7 nM. [2]In C57BL/6 mice, AZD3839 (69 mg/kg, p.o.) causes a dose- and time-dependent reduction of plasma and brain Aβ. In guinea pig and non-human primates, AZD3839 also inhibits Aβ generation.

For research and scientific purpose only, not for human use.

Cyclo(RGDyK)|cas 250612-42-1|DC Chemicals

Cyclo(RGDyK)|cas 250612-42-1|DC Chemicals

Cyclo(RGDyK) is a potent and selective αVβ3 integrin inhibitor with IC50 of 20 nM.

Product Name: Cyclo(RGDyK) |Catalog Number:  DC8399 | cas: 250612-42-1 | Other names:  | Chemical name:cyclo(L-arginylglycyl-L-α-aspartyl-D-tyrosyl-L-lysyl), 2,2,2-trifluoroacetate (1:2) | Molecule Formula: C31H43F6N9O12 | MW: 847.72

Cyclo(RGDyK) shows high affinity and selectivity for αVβ3 over αVβ5 and αIIbβ3. [1] Cyclo(RGDyK)-conjugated micelles (TPM) facilitated the cell-specific uptake of DiI into B16-F10 cells and HUVECs via integrin-mediated endocytosis compared with Cyclo(RGDyK) -free micelles (NPM). [2]In apoE−/− mice, Cyclo(RGDyK) (1 nmol, i.v.) inhibits the increase of αVβ3 integrin expression in the intima of the left stenotic carotid artery.

For research and scientific purpose only, not for human use.

NPS-1034|cas 1221713-92-3|DC Chemicals

NPS-1034|cas 1221713-92-3|DC Chemicals

NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

Product Name: NPS-1034 |Catalog Number:  DC8398 | cas: 1221713-92-3 | Other names:  | Chemical name:N-(3-fluoro-4-(3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide | Molecule Formula: C31H23F2N5O3 | MW: 551.54

In HCC827/GR cells, NPS-1034 does not show significant antiproliferative effects, while overcomes gefitinib resistance by inhibiting the phosphorylation of MET, Akt, and Erk. In H820 cells, NPS-1034 enhances sensitivity to EGFR-TKIs. In HCC78 cells, NPS-1034 inhibits ROS1 activity and cell proliferation. In addition, a combination of gefitinib and NPS-1034 enhances cell death by inducing caspase-3 and PARP-1 cleavage. [1] NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET, with IC50 of 112.7 and 190.3 nmol, respectively. [2]In SCID mice bearing HCC827/GR tumor xenografts, NPS-1034 (10 mg/kg, p.o.) decreases tumor growth, and the combination of gefitinib and NPS-1034 results in enhanced tumor growth inhibition via the inhibition of tumor proliferation and the induction of apoptosis. [1] In nude mice bearing MKN45 xenograft tumors, NPS-1034 (30 mg/kg, p.o.) decreases tumor growth through the inhibition of angiogenesis and the promotion of apoptosis.

For research and scientific purpose only, not for human use.


AMG 925|cas 1401033-86-0|DC Chemicals

AMG 925|cas 1401033-86-0|DC Chemicals

AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell.

Product Name: AMG 925 |Catalog Number:  DC8397 | cas: 1401033-86-0 | Other names: AMG 925,AMG925,AMG-925 | Chemical name:1-[7,8-dihydro-2-[[9-(trans-4-methylcyclohexyl)-9H-pyrido[4',3':4,5]pyrrolo[2,3-d]pyrimidin-2-yl]amino]-1,6-naphthyridin-6(5H)-yl]-2-hydroxy-ethanone | Molecule Formula: C26H29N7O2 | MW: 471.55

For research and scientific purpose only, not for human use.

Dyngo-4a|cas 1256493-34-1|DC Chemicals

Dyngo-4a|cas 1256493-34-1|DC Chemicals

Dyngo-4a is a potent dynamin inhibitor with IC50 of 0.38 μM, 1.1 μM, and 2.3 μM for DynI (brain), DynI (rec), and DynII (rec), respectively.

Product Name: Dyngo-4a |Catalog Number:  DC8396 | cas: 1256493-34-1 | Other names:  | Chemical name:(E)-N'-(2,4,5-trihydroxybenzylidene)-3-hydroxy-2-naphthohydrazide | Molecule Formula: C18H14N2O5 | MW: 338.31

Dyngo-4a inhibits dynamin-dependent endocytosis of transferrin in multiple cell types with IC₅₀ of 5.7 μM, and reduces synaptic vesicle endocytosis and activity-dependent bulk endocytosis in cultured neurons and synaptosomes. [1] In motor nerve terminals and cultured hippocampal neurons, Dyngo-4a blocks Alexa Fluor 488-BoNT/A-Hc internalization. [2] In Drosophila S2R+ cells, Dyngo-4a causes a decrease in the level of Armadillo/β-catenin.

For research and scientific purpose only, not for human use.

PF-4989216|cas 1276553-09-3|DC Chemicals

PF-4989216|cas 1276553-09-3|DC Chemicals

PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively.

Product Name: PF-4989216 |Catalog Number:  DC8395 | cas: 1276553-09-3 | Other names: PF-4989216,PF 4989216,PF4989216 | Chemical name:4-(4-cyano-2-fluorophenyl)-2-morpholino-5-(2H-1,2,4-triazol-3-yl)thiophene-3-carbonitrile | Molecule Formula: C18H13FN6OS | MW: 380.4

PF-4989216 significantly inhibits cell viability in SCLC cells with a PIK3CA mutation, such as NCI-H69, NCI-H1048, and Lu99A cells. PF-4989216, via PI3K signaling inhibition, blocks cell-cycle progression and reduces cell transformation in SCLCs. In SCLCs with PIK3CA mutation, PF-4989216 induces BIM-mediated apoptosis. [1]In SCID mice bearing NCI-H69 or NCI-H1048 xenograft tumors, PF-4989216 (350 mg/kg, p.o.) inhibits PI3K phosphorylation signaling and induces antitumor activity.

For research and scientific purpose only, not for human use.

Dibutyryl-cAMP (Bucladesine)|cas 16980-89-5|DC Chemicals

Dibutyryl-cAMP (Bucladesine)|cas 16980-89-5|DC Chemicals

Dibutyryl-cAMP (Bucladesine) is a cell-permeable PKA activator by mimicing the action of endogenous cAMP.

Product Name: Dibutyryl-cAMP (Bucladesine) |Catalog Number:  DC8394 | cas: 16980-89-5 | Other names:  | Chemical name:N-(1-oxobutyl)-cyclic 3',5'-(hydrogen phosphate) 2'-butanoate-adenosine,sodium salt (1?) | Molecule Formula: C18H23N5NaO8P | MW: 491.37

Dibutyryl-cAMP inhibits neuronal glucose uptake via PKA activation. [1] In cultured rat hepatocytes, Dibutyryl-cAMP inhibits inducible nitric oxide synthase expression and NF-kappaB-binding activity. [2] Dibutyryl-cAMP also suppress TNFalpha-induced hepatocyte apoptosis by inhibiting FADD up-regulation. [3]In a mouse model, bucladesine (600 nM/mouse, i.p.) reverses zinc chloride- and lead acetate-induced avoidance memory retention impairments.

For research and scientific purpose only, not for human use.

UM171|cas 1448724-09-1|DC Chemicals

UM171|cas 1448724-09-1|DC Chemicals

  UM171 is a potent agonist of human hematopoietic stem cell renewal, independently of AhR suppression.

Product Name: UM171 |Catalog Number:  DC8393 | cas: 1448724-09-1 | Other names:  | Chemical name:trans-N1-(2-benzyl-7-(2-methyl-2H-tetrazol-5-yl)-9H-pyrimido[4,5-b]indol-4-yl)cyclohexane-1,4-diamine | Molecule Formula: C25H27N9 | MW: 453.54

UM171 potently expands human CD34+CD45RA− mobilized peripheral blood (mPB) cells, attenuates cell differentiation and promotes ex vivo expansion of primitive human hematopoietic cells. [1]

For research and scientific purpose only, not for human use.

BQ-123|cas 136553-81-6|DC Chemicals

BQ-123|cas 136553-81-6|DC Chemicals

BQ-123 is a selective endothelin A receptor (ETA) antagonist with IC50 of 7.3 nM. Phase 2.

Product Name: BQ-123 |Catalog Number:  DC8392 | cas: 136553-81-6 | Other names: BQ-123,BQ 123,BQ123 | Chemical name:cyclo-Asp-Pro-Val-Leu-Trp | Molecule Formula: C31H42N6O7 | MW: 610.7

In porcine aortic vascular smooth muscle cells, BQ-123 selectively inhibits ETA-mediated contraction. [1] In rat vascular smooth muscle cells, BQ-123 inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis. [2]In rats, BQ-123 (1 mg/kg, i.v.) ameliorates myocardial ischemic-reperfusion injury. [3] In rats with pentylenetetrazole (PTZ)-induced tonic-clonic seizures, BQ-123 (3 mg/kg, i.v.) potently impedes the formation and spread of seizure. [4] In pregnant C57BL/6 mice, BQ-123 (6.7 mg/kg, i.p.) prevents LPS-induced preterm birth in mice via the induction of uterine and placental IL-10.

For research and scientific purpose only, not for human use.

Smoothened Agonist (SAG) HCl|cas 912545-86-9(free base)|DC Chemicals

Smoothened Agonist (SAG) HCl|cas 912545-86-9(free base)|DC Chemicals

Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.

Product Name: Smoothened Agonist (SAG) HCl |Catalog Number:  DC8391 | cas: 912545-86-9(free base) | Other names:  | Chemical name:N-(3-(pyridin-4-yl)benzyl)-3-chloro-N-((1r,4r)-4-(methylamino)cyclohexyl)benzo[b]thiophene-2-carboxamide hydrochloride | Molecule Formula: C28H29Cl2N3OS | MW: 526.52

SAG regulates Smo activity by binding directly to the Smo heptahelical bundle. [1] SAG induces Smo-dependent signaling through Gli in a GRK2-dependent way. [2] SAG also (1 nM) induces proliferation of neuronal and glial precursors without affecting the differentiation pattern of newly produced cells. [3]In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. [3] In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities.

For research and scientific purpose only, not for human use.

Oltipraz|cas 64224-21-1|DC Chemicals

Oltipraz|cas 64224-21-1|DC Chemicals

Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.

Product Name: Oltipraz |Catalog Number:  DC8390 | cas: 64224-21-1 | Other names:  | Chemical name:4-methyl-5-(pyrazin-2-yl)-3H-1,2-dithiole-3-thione | Molecule Formula: C8H6N2S3 | MW: 226.34

Oltipraz, as a chemoprotective agent, induces Phase II detoxification enzyme activity in a Nrf2-dependent manner. [1] In human HT29 colon cancer cells, oltipraz inhibits the induction of HIF-1α by insulin, hypoxia or CoCl2 by significantly accelerating degradation of HIF-1α protein. [2]Oltipraz (500 mg/kg, p.o.) significantly reduces multiplicity of gastric neoplasia in wild-type mice by 55%, but has no effect on tumor burden in nrf2-deficient mice. [1] In BALB/c nude mice transplanted with HCT116 cells, Oltipraz (200 mg/kg, p.o.) inhibits tumor growth and angiogenesis via inhibition of HIF-1α. [2] In rats on a CDAA diet, Oltipraz attenuate the progression of nonalcoholic steatohepatitis-related fibrosis.

For research and scientific purpose only, not for human use.

Detomidine hydrochloride|Detomidine hydrochloride|DC Chemicals

Detomidine hydrochloride|Detomidine hydrochloride|DC Chemicals
Detomidine hydrochloride produce dose-dependent sedative and analgesic effects, is a nonnarcotic, synthetic α2-adrenergic agonist

Catlog: DC8097| Product name: Detomidine hydrochloride| Cas: 90038-01-0| Other names: Detomidine hydrochloride| Molecule Formula: C12H15ClN2| MW: 222.71. Purity: >98%

Price: 100mg: 350 USD; 250mg: 500 USD; 1000mg: 1200 USD

Detomidine is an imidazole derivative and α2-adrenergic agonist, used as a large animal sedative, primarily used in horses. It is usually available as the salt detomidine hydrochloride. It is a prescription medication available to veterinarians sold under the trade name Dormosedan. Currently, detomidine is only licenced for use in horses.
Detomidine is a sedative with analgesic properties. α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors, thus inducing a negative feedback response, reducing production of excitatory neurotransmitters. Due to inhibition of the sympathetic nervous system, detomidine also has cardiac and respiratory effects and an antidiuretic action.

For research and scientific purpose only, not for human use.

Epacadostat (INCB024360)|cas 1204669-58-8|DC Chemicals

Epacadostat (INCB024360)|cas 1204669-58-8|DC Chemicals

Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM. Phase 2.

Product Name: Epacadostat (INCB024360) |Catalog Number:  DC8389 | cas: 1204669-58-8 | Other names: INCB024360,INCB-024360,INCB 024360 | Chemical name:[C(Z)]-4-[[2-[(aminosulfonyl)amino]ethyl]amino]-N-(3-bromo-4-fluorophenyl)-N'-hydroxy-1,2,5-oxadiazole-3-carboximidamide | Molecule Formula: C11H13BrFN7O4S | MW: 438.23

In IFN-γ–treated human HeLa cells, INCB024360 potently inhibits kynurenine production. INCB024360 also promotes T and natural killer (NK)-cell growth, increases IFN-gamma production, and reduces conversion to regulatory T (T(reg))-like cells. [1INCB024360 (100 mg/kg, p.o.), via IDO1 inhibition, suppresses kyn generation and tumor growth in immunocompetent, but not immunodeficient, mice. [1] In mice bearing CT26 colon carcinoma, INCB024360 (100 mg/kg, p.o.) also inhibits the growth of IDO-expressing tumors by reducing kynurenine.

For research and scientific purpose only, not for human use.

8-Bromo-cAMP|cas 76939-46-3|DC Chemicals

8-Bromo-cAMP|cas 76939-46-3|DC Chemicals

8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator.

Product Name: 8-Bromo-cAMP |Catalog Number:  DC8388 | cas: 76939-46-3 | Other names:  | Chemical name:8-bromoadenosine 3',5'-cyclic monophosphate sodium salt | Molecule Formula: C10H10BrN5NaO6P | MW: 430.08

8-Bromo-cAMP improves the reprogramming efficiency of human neonatal foreskin fibroblast (HFF1) cells. [1] In bronchial epithelial cells, 8-Bromo-cAMP decreases HDE-stimulated tumor necrosis factor (TNF)-α-converting enzyme (TACE; ADAM-17) activity and subsequent TNF-α release. [2]

For research and scientific purpose only, not for human use.

Bromodeoxyuridine (BrdU)|cas 59-14-3|DC Chemicals

Bromodeoxyuridine (BrdU)|cas 59-14-3|DC Chemicals

Bromodeoxyuridine (BrdU) is a nucleoside analog that competes with thymidine for incorporation into DNA, and used in the detection of proliferating cells.

Product Name: Bromodeoxyuridine (BrdU) |Catalog Number:  DC8386 | cas: 59-14-3 | Other names:  | Chemical name:5-bromo-1-((2R,4R,5R)-4-hydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)pyrimidine-2,4(1H,3H)-dione | Molecule Formula: C9H11BrN2O5 | MW: 307.1

In RG2 rat glioma cells, Bromodeoxyuridine induces a progressive, dose-responsive suppression of cancer cell line and cancer stem cell population expansion. In H9 cells and BJ fibroblasts, Bromodeoxyuridine alters the cell cycle profile. [1] BrdU is stably integrated into the DNA, and thus can be used in assessment of cell proliferation and other cell procession. [2]In rat glioma RG2 tumor model, Bromodeoxyuridine (300 mg/kg, i.p. or 0.8 mg/ml, p.o.) significantly slows tumor progression.

For research and scientific purpose only, not for human use.

Disodium (R)-2-Hydroxyglutarate|cas 103404-90-6|DC Chemicals

Disodium (R)-2-Hydroxyglutarate|cas 103404-90-6|DC Chemicals

Disodium (R)-2-Hydroxyglutarate is a competitive inhibitor of α-ketoglutarate-dependent dioxygenases with Ki of 0.628 mM.

Product Name: Disodium (R)-2-Hydroxyglutarate |Catalog Number:  DC8385 | cas: 103404-90-6 | Other names:  | Chemical name:sodium (R)-2-hydroxypentanedioate | Molecule Formula: C5H6Na2O5 | MW: 192.08

In U-87MG cells, (R)-2-Hydroxyglutarate acts as weak antagonists of α-KG to inhibit α-KG-dependent histone demethylases and increases dimethylation on both H3K9 and H3K79. [1] Besides, (R)-2-Hydroxyglutarate inhibits ATP synthase and mTOR signaling, and thus causes growth arrest and tumor cell killing. [2]

For research and scientific purpose only, not for human use.

Sodium Tauroursodeoxycholate (TUDC)|cas 35807-85-3|DC Chemicals

Sodium Tauroursodeoxycholate (TUDC)|cas 35807-85-3|DC Chemicals

Sodium Tauroursodeoxycholate (TUDC) is a water soluble bile salt, used for the treatment of gallstones and liver cirrhosis.

Product Name: Sodium Tauroursodeoxycholate (TUDC) |Catalog Number:  DC8384 | cas: 35807-85-3 | Other names:  | Chemical name:sodium 2-((R)-4-((3R,5S,7S,8R,9S,10S,13R,14S,17R)-3,7-dihydroxy-10,13-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentanamido)ethanesulfonate | Molecule Formula: C26H44NNaO6S | MW: 521.69

In vitro, Tauroursodeoxycholate shows protective and reversing effects on 17βEG-induced impairment of the cVA-of-CLF. [1] In Mz-ChA-1 cholangiocarcinoma cells, Tauroursodeoxycholate inhibits cell growth via Ca2+-, PKC-, and MAPK-dependent pathways. [3] In isolated rat hepatocytes, Tauroursodeoxycholate inhibits bile acid-Induced Apoptosis via a β1-integrin-mediated formation of cAMP. [4]In phalloidin-induced cholestasis rats, Tauroursodeoxycholate (360 μmol/kg, i.v.) significantly suppresses the decrease in bile flow and increases in serum alkaline phosphatase, leucine aminopeptidase and glutamic pyruvic transaminase activities, cholesterol, phospholipid and bile acid concentrations. [2]

For research and scientific purpose only, not for human use.

Dp44mT|cas 152095-12-0|DC Chemicals

Dp44mT|cas 152095-12-0|DC Chemicals

Dp44mT is a potent iron chelator, which shows selective antitumor activity.

Product Name: Dp44mT |Catalog Number:  DC8383 | cas: 152095-12-0 | Other names:  | Chemical name:2-(di-2-pyridinylmethylene)-N,N-dimethyl-hydrazinecarbothioamide | Molecule Formula: C14H15N5S | MW: 285.37

Dp44mT shows pronounced antiproliferative effects in SK-N-MC, SK-Mel-28, and MCF-7 cells with IC50 of 30 nM, 60 nM, and 60 nM, respectively, while no effects on normal MRC-5 fibroblasts. Dp44mT inhibits cellular Fe uptake from Fe-Tf in SK-N-MC neuroepithelioma and M109 cells, and induces cell apoptosis. [1] In MDA-MB-231 cells, Dp44mT specifically targets topoisomerase topo2α, and thus causes DNA damage. [2] Dp44mT, as a Pgp substrate, also overcomes multidrug resistance by the hijacking of lysosomal P-glycoprotein (Pgp). [3]In CD2F1 mice bearing M109 tumors, Dp44mT (0.4 mg/kg, i.v.) inhibits tumor growth in a dose-dependent manner. [1]

For research and scientific purpose only, not for human use.

PF-03084014 (PF3084014)|cas 1290543-63-3|DC Chemicals

PF-03084014 (PF3084014)|cas 1290543-63-3|DC Chemicals

PF-03084014 (PF-3084014) is a selective gamma-secretase inhibitor with IC50 of 6.2 nM in a cell-free assay. Phase 2.

Product Name: PF-03084014 (PF-3084014) |Catalog Number:  DC8382 | cas: 1290543-63-3 | Other names: PF03084014,PF 03084014,PF-03084014 | Chemical name:2-[[(2S)-6,8-difluoro-1,2,3,4-tetrahydro-2-naphthalenyl]amino]-N-[1-[2-[(2,2-dimethylpropyl)amino]-1,1-dimethylethyl]-1H-imidazol-4-yl]-(2S)-pentanamide | Molecule Formula: C27H41F2N5O | MW: 489.64

PF-03084014 inhibits Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1with IC50 of 13.3 nM. PF-03084014 downregulates Notch target genes Hes-1, and cMyc expression in HPB-ALL cells with IC50 of <1 nM and 10 nM, respectively. PF-03084014 inhibits cell growth of a subset of human T-ALL cell lines (HPB-ALL, DND-41, TALL-1,and Sup-T1) through induction of cell cycle arrest and apoptosis with IC50s of 30-100 nM. [1] PF-03084014 reduces proliferation of HUVECs with IC50 of 0.5 μM, and decreases the lumen formation with an IC50 value of 50 nM. PF-03084014 (1 μM) has no antiproliferative effect in MX1 cells; however, it inhibits migration by 95%. [2]PF-03084014 orally administrated in a single dose of 200 mg/kg, causes maximal NICD inhibition for ∼80% in xenograft HPB-ALL tumors. PF-03084014 shows robust antitumor activity in this mode with a maximal tumor growth inhibition of ∼ 92% at dose of 150 mg/kg, accompanied by a significant reduction of NICD/Notch1, tumor mitotic index (Ki67), and apoptosis (activated caspase-3) staining. [1] PF-03084014 (120 mg/kg) induces apoptosis, antiproliferation, reduces tumor cell self-renewal ability, impaires tumor vasculature, and decreases metastasis activity in breast cancer HCC1599 tumor-bearing mice. PF-03084014 treatment displays significant antitumor activity in various types of the breast xenograft models with TGI value of at least 50%. [2]

For research and scientific purpose only, not for human use.

PD-1/PD-L1 inhibitor 2|cas 1675203-84-5|DC Chemicals

PD-1/PD-L1 inhibitor 2|cas 1675203-84-5|DC Chemicals

PD-1/PD-L1 inhibitor 2 is a PD-1/PD-L1 interaction inhibitor with EC50 of 400 nM.

Product Name: PD-1/PD-L1 inhibitor 2 |Catalog Number:  DC8381 | cas: 1675203-84-5 | Other names: PD-L1 inhibitor 2,PD-1 inhibitor 2 | Chemical name:N-[2-[[[2-methoxy-6-[(2-methyl[1,1'-biphenyl]-3-yl)methoxy]-3-pyridinyl]methyl]amino]ethyl]-acetamide | Molecule Formula: C25H29N3O3 | MW: 419.52

For research and scientific purpose only, not for human use.

AZD8186|AZD-8186|PI3Kβand PI3Kδ inhibitor|DC Chemicals

AZD8186|AZD-8186|PI3Kβand PI3Kδ inhibitor|DC Chemicals

AZD8186 is and inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity.

Product Name: AZD8186 |Catalog Number:  DC8380 | cas: 1627494-13-6 | Other names: AZD8186,AZD-8186,AZD 8186 | Chemical name:(R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide | Molecule Formula: C24H25F2N3O4 | MW: 457.47

AZD8186 is and inhibitor of the beta isoform of phosphoinositide-3 kinase (PI3K), with potential antineoplastic activity. Upon administration, PI3Kbeta inhibitor AZD8186 selectively inhibits the activity of PI3Kbeta in the PI3K/Akt/mTOR signaling pathway, which may result in a decrease of tumor cell proliferation. It also induces cell death in PI3K-expressing cancer cells. By specifically targeting class I PI3K beta, this agent may be more efficacious and less toxic than pan PI3K inhibitors. PI3K-mediated signaling is often dysregulated in cancer cells and contributes to increased tumor cell growth, survival, and tumor resistance to a variety of antineoplastic agents. AZD8186 is currently under Phase I clinical trials.

For research and scientific purpose only, not for human use.

JH-II-127|LRRK2 inhibitor|DC Chemicals

JH-II-127|LRRK2 inhibitor|DC Chemicals

JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor.

Product Name: JH-II-127 |Catalog Number:  DC8379 | cas: 1700693-08-8 | Other names: 2-anilino-4-methylamino-5-chloropyrrolopyrimidine,JH-II127,JH-II 127 | Chemical name:2-anilino-4-methylamino-5-chloropyrrolopyrimidine | Molecule Formula: C19H21ClN6O3 | MW: 416.86

JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor,of both wild-type and G2019S mutant LRRK2.JH-II-127 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3 μM in a variety of cell types and is capable of inhibiting Ser935 phosphorylation in mouse brain following oral delivery of doses as low as 30 mg/kg.

For research and scientific purpose only, not for human use.

Mavatrep(JNJ-39439335)|TRPV1 inhibitor|DC Chemicals

Mavatrep(JNJ-39439335)|TRPV1 inhibitor|DC Chemicals

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.

Product Name: Mavatrep(JNJ-39439335) |Catalog Number:  DC8378 | cas: 956274-94-5 | Other names: JNJ-39439335,JNJ 39439335,JNJ39439335 | Chemical name: | Molecule Formula: C25H21F3N2O | MW: 422.44

Mavatrep is an orally bioavailable TRPV1 antagonist (Ki=6.5 nM), exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6.
in vitro: Mavatrep exhibits superior pharmacodynamic properties. In a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels, Mavatrep antagonizes capsaicin-induced Ca2+ influx, with an IC50 value of 4.6 nM. Mavatrep blocks the activation of hTRPV1 channels by Capsaicin (1 μM) and by pH (5.0) in a concentration-dependent fashion, with IC50 values of 23 and 6.8 nM, respectively.
in vivo: Mavatrep exhibits superior pharmacodynamic properties in the CFA model of inflammatory pain.

For research and scientific purpose only, not for human use.

CC-115|CC115|TOPK/DNA-PK inhibitor|DC Chemicals

CC-115|CC115|TOPK/DNA-PK inhibitor|DC Chemicals

CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.

Product Name: CC-115 |Catalog Number:  DC8377 | cas: 1228013-15-7 | Other names: CC115,CC 115 | Chemical name: | Molecule Formula: C16H16N8O | MW: 336.35

A dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity. CC-115 binds to and inhibits the activity of DNA-PK and both raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2), which may lead to a reduction in cellular proliferation of cancer cells expressing DNA-PK and TOR. DNA-PK, a serine/threonine kinase and a member of the PI3K-related kinase subfamily of protein kinases, is activated upon DNA damage and plays a key role in repairing double-stranded DNA breaks via the DNA nonhomologous end joining (NHEJ) pathway; mTOR, a serine/threonine kinase that is upregulated in a variety of tumors, plays an important role downstream in the PI3K/Akt/mTOR signaling pathway.

For research and scientific purpose only, not for human use.

TAS-301|TAS301|193620-69-8|DC Chemicals

TAS-301|TAS301|193620-69-8|DC Chemicals

TAS-301 is an inhibitor of smooth muscle cell migration and proliferation.

Product Name: TAS-301 |Catalog Number:  DC8376 | cas: 193620-69-8 | Other names: TAS-301,TAS 301.TAS301 | Chemical name:3-[Bis(4-methoxyphenyl)methylene]-1,3-dihydro-2H-indol-2-one | Molecule Formula: C23H19NO3 | MW: 357.4

Inhibitor of smooth muscle cell migration and proliferation. Blocks voltage-independent calcium influx and downstream PKC signaling. Inhibits neointimal thickening after balloon catheter injury to the rat common carotid artery.

For research and scientific purpose only, not for human use.

GLPG0634 (analog)|JAK inhibitor|DC Chemicasl

GLPG0634 (analog)|JAK inhibitor|DC Chemicasl

GLPG0634 (analog) is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be found in the reference patents.

Product Name: GLPG0634 analogue |Catalog Number:  DC8375 | cas: 1206101-20-3 | Other names:  | Chemical name:N-[5-[4-[(6-cyano-3-pyridinyl)methoxy]phenyl][1,2,4]triazolo[1,5-a]pyridin-2-yl]-cyclopropanecarboxamide | Molecule Formula: C23H18N6O2 | MW: 410.43

GLPG0634 (analog) is a pan JAK inhibitor with IC50s of 50-200 nM for JAK1/JAK2/JAK3; more information can be found in the reference patents.

For research and scientific purpose only, not for human use.

AG221|AG 221|mutated IDH2 inhibitor|DC Chemicals

AG221|AG 221|mutated IDH2 inhibitor|DC Chemicals

AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.

Product Name: AG-221 |Catalog Number:  DC8374 | cas: 1446502-11-9 | Other names: AG221,AG 221 | Chemical name: | Molecule Formula: C19H17F6N7O | MW: 473.14

AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein, making it a highly targeted investigational medicine for the potential treatment of patients with cancers that harbor an IDH2 mutation. AG-221 has received orphan drug and fast track designations from the U.S. FDA. In September 2013, Agios initiated a Phase 1 multicenter, open-label, dose escalation clinical trial of AG-221 designed to assess the safety and tolerability of AG-221 in advanced hematologic malignancies. In October 2014, Agios initiated four expansion cohorts as part of the ongoing Phase 1 study and expanded its development program with the initiation of a Phase 1/2 study of AG-221 in advanced solid tumors.

For research and scientific purpose only, not for human use.

GSK-8573|GSK8573|Inactive control of GSK-2801|DC Chemicals

GSK-8573|GSK8573|Inactive control of GSK-2801|DC Chemicals

GSK-8573 is the inactive control of GSK-2801.

Product Name: GSK-8573 |Catalog Number:  DC8373 | cas: 1693766-04-9 | Other names: gsk-5873,gsk5873 | Chemical name:1-(1-(3-methoxyphenyl)-7-propoxyindolizin-3-yl)ethan-1-one | Molecule Formula: C20H21NO3 | MW: 323.39

GSK8573 is the inactive control of GSK-2801.

For research and scientific purpose only, not for human use.

Vildagliptin (LAF-237; NVP-LAF 237)|DC Chemcials

Vildagliptin (LAF-237; NVP-LAF 237)|DC Chemcials

Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.

Product Name: Vildagliptin |Catalog Number:  DC8371 | cas: 274901-16-5 | Other names: LAF237; Galvus; NVP-LAF 237; Zomelis | Chemical name: | Molecule Formula: C17H25N3O2 | MW: 303.4

Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.
in vitro: Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 ?mol/L [1].
in vivo: Compared to age-, gender-, BMI-matched subjects with normal renal function, the mean AUC of vildagliptin after 14 days in patients with mild, moderate, and severe RI increased by 40%, 71%, and 100%, respectively. The treatment was effective in modulating stress in pancreatic tissue, both by reducing levels of stress markers as well as by increasing activity of SOD and catalase. After analyzing the pancreatic histology, we found that vildagliptin was also able to preserve islets and pancreatic β-cells, especially at the concentration of 5 mg/kg.

For research and scientific purpose only, not for human use.

Teneligliptin|CAS No:760937-92-6|DC Chemicals

Teneligliptin|CAS No:760937-92-6|DC Chemicals

Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.

Product Name: Teneligliptin hydrobromide |Catalog Number:  DC8370 | cas: 906093-29-6 | Other names:  | Chemical name: | Molecule Formula: C44H65Br5N12O2S2 | MW: 1257.72

Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.
in vitro: Teneligliptin is a novel chemotype prolylthiazolidine-based DPP-4 inhibitor. The present study aimed to characterize the pharmacological profiles of teneligliptin in vitro and in vivo. Teneligliptin competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC(50) values of approximately 1 nmol/l [1].
in vivo: Oral administration of teneligliptin in Wistar rats resulted in the inhibition of plasma DPP-4 with an ED(50) of 0.41 mg/kg. Plasma DPP-4 inhibition was sustained even at 24h after administration of teneligliptin. An oral carbohydrate-loading test in Zucker fatty rats showed that teneligliptin at ≥ 0.1mg/kg increased the maximum increase in plasma glucagon-like peptide-1 and insulin levels, and reduced glucose excursions. Six-weeks-old C57BL/6N mice were fed a high-fat diet (60%kcal fat) ad libitum and administered teneligliptin (30 or 60mg/kg) via drinking water for 10 weeks. Mice fed a high-fat diet showed accelerated body weight gain.

For research and scientific purpose only, not for human use.

Eltrombopag olamine|c-mpl agonist|DC Chemicals

Eltrombopag olamine|c-mpl agonist|DC Chemicals

Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis.

Product Name: Eltrombopag olamine |Catalog Number:  DC8369 | cas: 496775-62-3 | Other names: Eltrombopag diethanolamine salt; Promacta; Revolade; SB-497115GR | Chemical name: | Molecule Formula: C29H36N6O6 | MW: 564.63

Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis.
IC50 Value: 0.27 uM (EC50 in murine BAF3 cells)
Potential advantages of eltrombopag may include a sustained platelet response and a good tolerability profile.
in vitro: Eltrombopag demonstrated a half maximal effective concentration (EC50) of 0.27 uM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR) [1]. Eltrombopag stimulates the growth of TPO-dependent cell lines via JAK2 and STAT signaling pathways and stimulates isolated human CD34+ cells to become megakaryocytes and produce platelets.
in vivo: Twelve weeks of antiviral therapy, with concurrent receipt of eltrombopag or placebo, were completed by 36%, 53%, and 65% of patients receiving 30 mg, 50 mg, and 75 mg of eltrombopag, respectively, and by 6% of patients in the placebo group [3]. Eltrombopag was administered as once-daily oral capsules for 10 days at doses of 5, 10, 25, 30, 50, and 75 mg. The pharmacokinetics of eltrombopag was dose dependent and linear, and eltrombopag increased platelet counts in a dose-dependent manner.
Toxicity: There were no apparent differences in the incidence or severity of adverse events in subjects receiving active or placebo study medication [4]. Long-term treatment with eltrombopag was generally safe, well tolerated, and effective in maintaining platelet counts in the desired range.
Clinical trial: Eltrombopag In Cord Blood Or Haploidentical Bone Marrow Transplantation.

For research and scientific purpose only, not for human use.

BIO-Acetoxime|GSK-3 inhibitor|DC Chemicals

BIO-Acetoxime|GSK-3 inhibitor|DC Chemicals

BIO-Acetoxime is an analog of the GSK3 inhibitor 6-bromoindirubin-3’-oxime, or BIO

Product Name: BIO-Acetoxime |Catalog Number:  DC8368 | cas: 740841-15-0 | Other names: GSK3 Inhibitor X
6-Bromoindirubin-3'-acetoxime | Chemical name:(2'Z,3'E)-6-Bromoindirubin-3'-acetoxime | Molecule Formula: C18H12BrN3O3 | MW: 398.21

BIO-Acetoxime is an analog of the GSK3 inhibitor 6-bromoindirubin-3’-oxime, or BIO.It potently inhibits GSK3α/β (IC50 = 10 nM), with selectivity over Cdk5/p25, Cdk2/A, and Cdk1/B (IC50s = 2.4, 4.3, and 63 µM, respectively).BIO-Acetoxime has been used to study the role of GSK3 in the Wnt/β-catenin pathway.3 It also suppresses the cytopathic effects of herpes viruses and reduces viral yields in human oral epithelial cells.

For research and scientific purpose only, not for human use.

IN00076730|cas 1454700-89-0|DC Chemicals

IN00076730|cas 1454700-89-0|DC Chemicals

Product Name: IN00076730 |Catalog Number:  DC8367 | cas: 1454700-89-0 | Other names:  | Chemical name:Spiro[cyclohexane-1,2'-[2H]inden]-3'(1'H)-one, 5'-bromo-4-methoxy-3,5-dimethyl-, (1α,3R,4β,5S)-rel-  | Molecule Formula: C17H21BrO2  | MW: 337.25

For research and scientific purpose only, not for human use.

ALS-22335,ALS 22335,ALS22335|DC Chemicals

ALS-22335,ALS 22335,ALS22335|DC Chemicals

Product Name: ALS-22335 |Catalog Number:  DC8366 | cas: N/A | Other names: ALS-22335,ALS 22335,ALS22335 | Chemical name: | Molecule Formula: C23H31FN3O10P | MW: 559.48

For research and scientific purpose only, not for human use.

TP 353,TP353|DC Chemicals

TP 353,TP353|DC Chemicals

Product Name: TP-353 |Catalog Number:  DC8365 | cas: N/A | Other names: TP 353,TP353 | Chemical name:phenyl 2-(benzyloxy)-3-
(dibenzylamino)-5-fluoro-6-
methylbenzoate | Molecule Formula: C35H30FNO3 | MW: 531.62

For research and scientific purpose only, not for human use.

TP-808(TP808),CAS 852821-06-8 from DC Chemicals

TP-808(TP808),CAS 852821-06-8 from DC Chemicals

Product Name: TP-808 |Catalog Number:  DC8364 | cas: 852821-06-8 | Other names: TP808,TP 808 | Chemical name:(4aS,8aS,9S)-9-(Dimethylamino)-4a-[[(1,1-dimethylethyl)dimethylsilyl]oxy]-8a,9-dihydro-3-(phenylmethoxy)-naphth[2,3-d]isoxazole-4,5(4aH,8H)-dione | Molecule Formula: C26H34N2O5Si | MW: 482.64

For research and scientific purpose only, not for human use.


L-779,450|L-779450|RAF inhibitor|DC Chemicals

L-779,450|L-779450|RAF inhibitor|DC Chemicals

L-779,450 is a potent, ATP-competitive Raf (Raf kinase) inhibitor (IC50 = 10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.

Product Name: L-779,450 |Catalog Number:  DC8362 | cas: 303727-31-3 | Other names:  | Chemical name:2-Chloro-5-[2-Phenyl-5-(4-pyridinyl)-1H-imidazol-4-yl]phenol | Molecule Formula: C20H14ClN3O | MW: 347.8

Potent, ATP-competitive Raf kinase inhibitor (IC50 = 10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.

For research and scientific purpose only, not for human use.

CDDO(Bardoxolone; RTA 401)|DC Chemicals

CDDO(Bardoxolone; RTA 401)|DC Chemicals

CDDO is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM.

Product Name: CDDO(Bardoxolone; RTA 401) |Catalog Number:  DC8361 | cas: 218600-44-3 | Other names:  | Chemical name:2-cyano-3,12-dioxo-oleana-1,9(11)-dien-28-oic acid | Molecule Formula: C31H41NO4 | MW: 491.66

CDDO is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM.By suppressing reactive oxygen and nitrogen species (ROS/RNS) formation, it promotes the cellular control of ROS/RNS levels that would lead to DNA damage associated with tumorigenesis.In various cancer cell lines, CDDO has been shown to specifically inhibit proliferation and induce apoptosis.Mechanism studies revealed that CDDO is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.

For research and scientific purpose only, not for human use.

GSK-5959|BRPF1 bromodomain inhibitor|DC Chemicals

GSK-5959|BRPF1 bromodomain  inhibitor|DC Chemicals

GSK 5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).

Product Name: GSK 5959 |Catalog Number:  DC8360 | cas: 901245-65-6 | Other names: GSK5959,GSK-5959 | Chemical name:N-[2,3-dihydro-1,3-dimethyl-2-oxo-6-(1-piperidinyl)-1H-benzimidazol-5-yl]-2-methoxy-benzamide | Molecule Formula: C22H26N4O3 | MW: 394.5

The bromodomain and PHD finger-containing (BRPF) proteins are scaffolding components of chromatin-binding MOZ/MORF histone acetyltransferase complexes, which have activity as transcriptional regulators.BRPF1 (BR140 or Peregrin) is important for maintaining Hox gene expression and the development of multiple tissues, axial skeleton, and the hematopoietic system.GSK 5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).It exhibits greater than 100-fold selectivity for the BRPF1 bromodomain over a panel of 35 other bromodomains. GSK 5959 disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3

For research and scientific purpose only, not for human use.

STF-31|STF31|GLUT1 inhibitor|DC Chemicals

STF-31|STF31|GLUT1 inhibitor|DC Chemicals

STF-31 is an inhibitor of GLUT1 (IC50 = ~1 µM) that blocks glucose uptake.

Product Name: STF-31 |Catalog Number:  DC8359 | cas: 724741-75-7 | Other names: STF31,STF 31 | Chemical name:4-[[[[4-(1,1-dimethylethyl)phenyl]sulfonyl]amino]methyl]-N-3-pyridinyl-benzamide | Molecule Formula: C23H25N3O3S | MW: 423.5

STF-31 is an inhibitor of GLUT1 (IC50 = ~1 µM) that blocks glucose uptake.It induces necrosis in cancer cells that lack the von Hippel-Lindau tumor suppressor gene, which overexpress GLUT1.Although STF-31 binds GLUT1, suggesting a direct effect, STF-31 also inhibits nicotinamide phosphoribosyltransferase, an enzyme that induces GLUT1 expression. STF-31 is also toxic to human pluripotent stem cells (hPSCs) and can be used to selectively eliminate hPSCs from mixed cultures.

For research and scientific purpose only, not for human use.

ONO-4059(ONO-WG-307)|Btk/Tec inhibitor|DC Chemicals

ONO-4059(ONO-WG-307)|Btk/Tec inhibitor|DC Chemicals

ONO-4059 is a novel Small Molecule Dual Inhibitor Of Bruton’s Tyrosine Kinase (Btk) and Tec Kinase.

Product Name: ONO-4059 |Catalog Number:  DC8358 | cas: 1351635-67-0 | Other names: ONO-4059,ONO 4059,ONO4059 | Chemical name:(S)-9-(1-acryloylpiperidin-3-yl)-6-amino-7-(4-phenoxyphenyl)-7H-purin-8(9H)-one | Molecule Formula: C25H24N6O3 | MW: 456.5

ONO-4059 is a highly potent and dual oral Btk/Tec inhibitor with an IC50 in the sub-nmol/L range. Previous studies with ONO-4059 demonstrated that ONO-4059 significantly inhibits the macrophage colony-stimulating factor (M-CSF) and receptor activator of nuclear factor-κB ligand (RANKL)-driven osteoclast defferentiation. The treatment with ONO-4059 also resulted in a dose-dependent inhibition of arthritis severity and bone damage in a mouse collagen induced arthritis (CIA) model (ACR 2012).Btk and Tec are required for osteoclast differentiation and activation based on the genetic evidence obtained from Btk and Tec double deficient mice. Dual Btk/Tec inhibitor, ONO-4059 may be a novel therapeutic target for RA to suppress bone erosion and inflammation.

For research and scientific purpose only, not for human use.


Losartan carboxylic acid|EXP-3174|DC Chemicals

Losartan carboxylic acid|EXP-3174|DC Chemicals

Losartan carboxylic acid is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver.

Product Name: Losartan Carboxylic Acid |Catalog Number:  DC8356 | cas: 124750-92-1 | Other names: E-3174,EXP-3174,E 3174,EXP 3174,E3174,EXP3174 | Chemical name:2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid | Molecule Formula: C22H21ClN6O2 | MW: 436.89

Losartan carboxylic acid is a physiologically active metabolite of losartan, produced by cytochrome P450 isoforms in the liver.Like the parent compound, losartan carboxylic acid is a potent AT1 antagonist (Kis = 0.57 and 0.67 nM for rat and human forms, respectively), producing a depressor response and vasodilatation.When administered intravenously, losartan carboxylic acid is more potent and has a longer duration of action than losartan.8 However, the metabolite has very low oral bioavailability.Losartan, but not its metabolite, inhibits platelet aggregation in vitro.

For research and scientific purpose only, not for human use.