TCS 5861528|TRPA1 channel blocker|DC Chemials
TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx.
Product name: TCS 5861528 |Cat No. DC8262|Other names: TCS 5861528 ,TCS 5861528,TCS 5861528 |Cas: 332117-28-9|Molecule Weight: 369.42|Molecule Formular: C19H23N5O3| Purity: >98%
Selective TRPA1 channel blocker (IC50 values are 14.3 and 18.7 µM for AITC- and 4-HNE- evoked Ca2+ influx respectively). Exhibits little of no activity at TRPV1 channels. Reduces mechanical hypersensitivity, attenuates diabetes mellitus hypersensitivity and displays antinociceptive properties.
For research and scientific purpose only, not for human use.
2015年6月25日星期四
(-)JQ-1|Negative of +JQ-1|DC CHEMICALS
(-)JQ-1|Negative of +JQ-1|DC CHEMICALS
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
Product name: (-)-JQ-1 |Cat No. DC8261|Other names: -JQ-1,-JQ-1 , -JQ-1 |Cas: 1268524-71-5|Molecule Weight: 457|Molecule Formular: C23H25ClN4O2S| Purity: >98%,ee>99%
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
For research and scientific purpose only, not for human use.
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
Product name: (-)-JQ-1 |Cat No. DC8261|Other names: -JQ-1,-JQ-1 , -JQ-1 |Cas: 1268524-71-5|Molecule Weight: 457|Molecule Formular: C23H25ClN4O2S| Purity: >98%,ee>99%
The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
For research and scientific purpose only, not for human use.
Exemestane(FCE 24304)|aromatase inhibitor|DC Chemicals
Exemestane(FCE 24304)|aromatase inhibitor|DC Chemicals
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
Product name: Exemestane(FCE 24304) |Cat No. DC8260|Other names: FCE24304 ,FCE-24304|Cas: 107868-30-4|Molecule Weight: 296.4|Molecule Formular: C20H24O2| Purity: >98%
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM. Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells.
Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats .Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors.
For research and scientific purpose only, not for human use.
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
Product name: Exemestane(FCE 24304) |Cat No. DC8260|Other names: FCE24304 ,FCE-24304|Cas: 107868-30-4|Molecule Weight: 296.4|Molecule Formular: C20H24O2| Purity: >98%
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM. Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells.
Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats .Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors.
For research and scientific purpose only, not for human use.
PF0477736|CHK inhibitor|DC Chemicals
PF0477736|CHK inhibitor|DC Chemicals
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
Product name: PF0477736 |Cat No. DC8259|Other names: PF 477736 ,PF-477736,PF477736 |Cas: 952021-60-2|Molecule Weight: 419.48|Molecule Formular: C22H25N7O2| Purity: >98%
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
For research and scientific purpose only, not for human use.
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
Product name: PF0477736 |Cat No. DC8259|Other names: PF 477736 ,PF-477736,PF477736 |Cas: 952021-60-2|Molecule Weight: 419.48|Molecule Formular: C22H25N7O2| Purity: >98%
PF 477736 is a CHK inhitor with Ki values of 0.49 and 47 nM for Chk1 and Chk2 respectively. A proprietary compound targeting cell cycle checkpoint kinase 1 (chk1) with potential chemopotentiation activity
For research and scientific purpose only, not for human use.
Baricitinib phosphate|JAK 1 inhibitor|DC Chemicals
Baricitinib phosphate|JAK 1 inhibitor|DC Chemicals
Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
Product name: Baricitinib phosphate |Cat No. DC8258|Other names: INCB-028050,LY-3009104,INCB 028050,LY 3009104,INCB028050,LY3009104|Cas: 1187595-84-1|Molecule Weight: 469.41|Molecule Formular: C16H20N7O6PS| Purity: >98%
Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.in vitro: INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. Significant efficacy, as assessed by improvements in clinical, histologic and radiographic signs of disease, was achieved in the rat adjuvant arthritis model with doses of INCB028050 providing partial and/or periodic inhibition of JAK1/JAK2 and no inhibition of JAK3.
in vivo: The efficacy following daily oral administration of INCB028050 was assessed at doses of 1, 3, or 10 mg/kg based on its pharmacokinetic profile in this species. Disease severity was assessed periodically, scoring clinical signs of disease. These doses were based on the PK/PD relationship established with the IL-6 WBA, with the goal of inhibiting JAK1/2 signaling by no more than 50% for half of the day. Relative to vehicle-treated animals, increasing doses of INCB028050 inhibited disease scores by 24% (p < 0.05), 57% (p < 0.01), and 81% (p < 0.01), respectively. Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies.
Clinical trial: Baricitinib (LY3009104, INCB28050) against JAK1/JAK2 starting phase IIb for rheumatoid arthritis
For research and scientific purpose only, not for human use.
Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.
Product name: Baricitinib phosphate |Cat No. DC8258|Other names: INCB-028050,LY-3009104,INCB 028050,LY 3009104,INCB028050,LY3009104|Cas: 1187595-84-1|Molecule Weight: 469.41|Molecule Formular: C16H20N7O6PS| Purity: >98%
Baricitinib phosphate(INCB 028050; LY 3009104) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2.in vitro: INCB028050 inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. Significant efficacy, as assessed by improvements in clinical, histologic and radiographic signs of disease, was achieved in the rat adjuvant arthritis model with doses of INCB028050 providing partial and/or periodic inhibition of JAK1/JAK2 and no inhibition of JAK3.
in vivo: The efficacy following daily oral administration of INCB028050 was assessed at doses of 1, 3, or 10 mg/kg based on its pharmacokinetic profile in this species. Disease severity was assessed periodically, scoring clinical signs of disease. These doses were based on the PK/PD relationship established with the IL-6 WBA, with the goal of inhibiting JAK1/2 signaling by no more than 50% for half of the day. Relative to vehicle-treated animals, increasing doses of INCB028050 inhibited disease scores by 24% (p < 0.05), 57% (p < 0.01), and 81% (p < 0.01), respectively. Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies.
Clinical trial: Baricitinib (LY3009104, INCB28050) against JAK1/JAK2 starting phase IIb for rheumatoid arthritis
For research and scientific purpose only, not for human use.
GNE 477|PI3K/mTOR inhibitor|DC Chemicals
GNE 477|PI3K/mTOR inhibitor|DC Chemicals
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
Product name: GNE 477 |Cat No. DC8257|Other names: GNE-477 ,GNE477 |Cas: 1032754-81-6|Molecule Weight: 504.63|Molecule Formular: C21H28N8O3S2| Purity: >98%
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.GNE-477 is a potent dual PI3K/mTOR inhibitor that displays desirable pharmacokinetic properties in each of three species studied. GNE-477 also exhibited stasis in a PC3 tumor growth inhibition study.
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.
Product name: GNE 477 |Cat No. DC8257|Other names: GNE-477 ,GNE477 |Cas: 1032754-81-6|Molecule Weight: 504.63|Molecule Formular: C21H28N8O3S2| Purity: >98%
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR.GNE-477 is a potent dual PI3K/mTOR inhibitor that displays desirable pharmacokinetic properties in each of three species studied. GNE-477 also exhibited stasis in a PC3 tumor growth inhibition study.
For research and scientific purpose only, not for human use.
AS 602801(Bentamapimod)|JNK Inhibitor|DC Chemicals
AS 602801(Bentamapimod)|JNK Inhibitor|DC Chemicals
AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.
Product name: AS 602801(Bentamapimod) |Cat No. DC8256|Other names: AS-602801 ,Bentamapimod ,AS602801|Cas: 848344-36-5|Molecule Weight: 457.55|Molecule Formular: C25H23N5O2S| Purity: >98%
AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.In activated PBMCs from HVs, we showed that AS602801 blocked T-lymphocyte proliferation and induced apoptosis. In RRMS CD4+ and CD8+ cells, AS602801 induced apoptosis genes and expression of surface markers, while in RRMS CD11b+ cells it induced expression of innate immunity receptors and co-stimulatory molecules. Untreated cells from RRMS active-phase patients significantly released interleukin-23 (IL-23) and interferon-gamma (IFN-γ) and expressed less apoptosis markers compared to the cells of HVs.
For research and scientific purpose only, not for human use.
AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.
Product name: AS 602801(Bentamapimod) |Cat No. DC8256|Other names: AS-602801 ,Bentamapimod ,AS602801|Cas: 848344-36-5|Molecule Weight: 457.55|Molecule Formular: C25H23N5O2S| Purity: >98%
AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.In activated PBMCs from HVs, we showed that AS602801 blocked T-lymphocyte proliferation and induced apoptosis. In RRMS CD4+ and CD8+ cells, AS602801 induced apoptosis genes and expression of surface markers, while in RRMS CD11b+ cells it induced expression of innate immunity receptors and co-stimulatory molecules. Untreated cells from RRMS active-phase patients significantly released interleukin-23 (IL-23) and interferon-gamma (IFN-γ) and expressed less apoptosis markers compared to the cells of HVs.
For research and scientific purpose only, not for human use.
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