Mequitazine |cas 29216-28-2
DC Chemicals, Website: www.dcchemicals.com
Product Name: Mequitazine|Cas Number: 29216-28-2| Catalog Number: DC10407
Mequitazine is a potent, nonsedative and long-acting histamine H1 antagonist.
Mequitazine is a potent H1-receptors selective antihistaminic drug widely studied and used for allergic disorders such as hay fever and urticaria[1]. Mequitazine demonstrates significant bactericidal effects against all the tested clinical isolates including Ps. aeruginosa. Its effect against the Gram-positive isolates is more pronounced[2].Mequitazine and clemizole antagonize the effect of histamine in guinea-pig ileum competitively. Mequitazine at 107 produces a parallel shift of the dose-response curve to acetylcholine in the rat duodenum. Mequitazine at highest concentration shows anticholinergic activity[3]. Mequitazine inhibits contractile responses to KCl, phenylephrine (PE), 5-hydroxytryptamine (5-HT), and Ca2+ in rat aorta[4].
2017年12月3日星期日
Imisopasem manganese|cas 218791-21-0
Imisopasem manganese|cas 218791-21-0
DC Chemicals, Website: www.dcchemicals.com
Product Name: Imisopasem manganese|Cas Number: 218791-21-0| Catalog Number: DC10406|Other Nmaes: M40403
Imisopasem manganese (M40403) is a stable non-peptidyl mimetic of manganese superoxide MnSOD.
M40403 is a small molecule, synthetic manganese containing superoxide dismutase mimetic (SODm) that removes superoxide anions without interfering with other reactive species known to be involved in inflammatory responses (e.g. nitric oxide, NO and peroxynitrite, ONOO-)[1].M40403 is a small-molecule superoxide dismutase mimetic that has shown efficacy in animal model disease states in which superoxide anions are thought to play a key role. M40403 inhibits the inflammatory response following the intrapleural injection of carrageenan in rats. All parameters of inflammation are attenuated by M40403 except for NOx, PGE2 and IL-10 which remains unaltered[1]. Decreased apoptosis of the large and particularly the small bowel and marked recovery of both lymphoid and hematopoietic tissues occurs in the M40403 pre-treated mice. M40403 is effective in reducing TBI-induced tissue destruction and has potential as a new radioprotective agent[2].
DC Chemicals, Website: www.dcchemicals.com
Product Name: Imisopasem manganese|Cas Number: 218791-21-0| Catalog Number: DC10406|Other Nmaes: M40403
Imisopasem manganese (M40403) is a stable non-peptidyl mimetic of manganese superoxide MnSOD.
M40403 is a small molecule, synthetic manganese containing superoxide dismutase mimetic (SODm) that removes superoxide anions without interfering with other reactive species known to be involved in inflammatory responses (e.g. nitric oxide, NO and peroxynitrite, ONOO-)[1].M40403 is a small-molecule superoxide dismutase mimetic that has shown efficacy in animal model disease states in which superoxide anions are thought to play a key role. M40403 inhibits the inflammatory response following the intrapleural injection of carrageenan in rats. All parameters of inflammation are attenuated by M40403 except for NOx, PGE2 and IL-10 which remains unaltered[1]. Decreased apoptosis of the large and particularly the small bowel and marked recovery of both lymphoid and hematopoietic tissues occurs in the M40403 pre-treated mice. M40403 is effective in reducing TBI-induced tissue destruction and has potential as a new radioprotective agent[2].
SPACE peptide
SPACE peptide
DC Chemicals, Website: www.dcchemicals.com
Product Name: SPACE peptide|Cas Number: | Catalog Number: DC10405|Other Nmaes: AC-TGSTQHQ-CG,Disulfide Bridge 2–10
SPACE peptide is a skin penetrating peptide which facilitates the delivery of molecules through the skin.
SPACE peptide, when conjugates to cargoes such as small molecules and proteins, is able to facilitate their penetration across the stratum corneum into epidermis and dermis. The peptide also exhibits increased penetration into various cells including keratinocytes, fibroblasts, and endothelial cells, likely through a macropinocytosis pathway[1]. SPACE enhances cyclosporine A, penetration into the skin significantly. It does not alter the skin lipid barrier. It interacts with skin proteins and induces changes in skin protein secondary structures (α-helices, β-sheet, random coils and turns). SPACE enhances cyclosporine A skin penetration, via a transcellular pathway, enhancing its partitioning into keratin-rich corneocytes through concurrent binding of SPACE with keratin and cyclosporine A. Interaction between SPACE and keratin best correlates with measured cyclosporine A skin transport[2]. SPACE-peptide in combination with a DOTAP-based ethosomal carrier system can enhance skin delivery of siRNA[3]. The SPACE-ethosomal system enhances hyaluronic acid penetration into porcine skin in vitro by 7.8+/−1.1-fold compared to PBS[4].The efficacy of DOTAP-SES in delivering GAPDH-siRNA into skin is confirmed in BALB/C mice. Topical application of DOTAP-SES on mice skin results in 63.2%±7.7% of GAPDH knockdown, which is significantly higher than that from GAPDH-siRNA PBS (p<0.05) [3].
DC Chemicals, Website: www.dcchemicals.com
Product Name: SPACE peptide|Cas Number: | Catalog Number: DC10405|Other Nmaes: AC-TGSTQHQ-CG,Disulfide Bridge 2–10
SPACE peptide is a skin penetrating peptide which facilitates the delivery of molecules through the skin.
SPACE peptide, when conjugates to cargoes such as small molecules and proteins, is able to facilitate their penetration across the stratum corneum into epidermis and dermis. The peptide also exhibits increased penetration into various cells including keratinocytes, fibroblasts, and endothelial cells, likely through a macropinocytosis pathway[1]. SPACE enhances cyclosporine A, penetration into the skin significantly. It does not alter the skin lipid barrier. It interacts with skin proteins and induces changes in skin protein secondary structures (α-helices, β-sheet, random coils and turns). SPACE enhances cyclosporine A skin penetration, via a transcellular pathway, enhancing its partitioning into keratin-rich corneocytes through concurrent binding of SPACE with keratin and cyclosporine A. Interaction between SPACE and keratin best correlates with measured cyclosporine A skin transport[2]. SPACE-peptide in combination with a DOTAP-based ethosomal carrier system can enhance skin delivery of siRNA[3]. The SPACE-ethosomal system enhances hyaluronic acid penetration into porcine skin in vitro by 7.8+/−1.1-fold compared to PBS[4].The efficacy of DOTAP-SES in delivering GAPDH-siRNA into skin is confirmed in BALB/C mice. Topical application of DOTAP-SES on mice skin results in 63.2%±7.7% of GAPDH knockdown, which is significantly higher than that from GAPDH-siRNA PBS (p<0.05) [3].
BIA 10-2474|cas 1233855-46-3
BIA 10-2474|cas 1233855-46-3
DC Chemicals, Website: www.dcchemicals.com
Product Name: BIA 10-2474|Cas Number: 1233855-46-3| Catalog Number: DC10404|Other Nmaes: BIA10-2474; BIA-10-2474
BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.
ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70mg/kg (i.p.) in various brain regions. IC50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus)[1].In January 2016, severe adverse events (SAE) occurs in the Phase I clinical trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought[2].
DC Chemicals, Website: www.dcchemicals.com
Product Name: BIA 10-2474|Cas Number: 1233855-46-3| Catalog Number: DC10404|Other Nmaes: BIA10-2474; BIA-10-2474
BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.
ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70mg/kg (i.p.) in various brain regions. IC50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus)[1].In January 2016, severe adverse events (SAE) occurs in the Phase I clinical trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought[2].
FAS-IN-1 Tosylate
FAS-IN-1 Tosylate
DC Chemicals, Website: www.dcchemicals.com
Product Name: FAS-IN-1 Tosylate|Cas Number: | Catalog Number: DC10403
FAS-IN-1 tosylate is a potent inhibitor of fatty acid synthase (FAS) extracted from patent WO 2012064642 A1, compound 29; has an IC50 of 10 nM.
DC Chemicals, Website: www.dcchemicals.com
Product Name: FAS-IN-1 Tosylate|Cas Number: | Catalog Number: DC10403
FAS-IN-1 tosylate is a potent inhibitor of fatty acid synthase (FAS) extracted from patent WO 2012064642 A1, compound 29; has an IC50 of 10 nM.
R121919 |cas 195055-03-9
R121919 |cas 195055-03-9
DC Chemicals, Website: www.dcchemicals.com
Product Name: R121919|Cas Number: 195055-03-9| Catalog Number: DC10401|Other Nmaes: NBI30775; R 121919; R-121919
R121919 is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
R121919 is a potent small-molecule CRF1 receptor antagonistwith high affinity for the CRF1 receptor (Ki=2–5 nM) and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types[1].R121919 reduces measures of both anxiety and depression in the depressed patients. R121919 dose dependently decreases adrenocorticopin hormone and corticosterone responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively[1]. R121919 reduces levels of anxiety in mice with a steep dose-response curve. Molecules such as GR, MR, BAG-1 and AP-1 have been identified as some of the drug's intracellular targets[2].
DC Chemicals, Website: www.dcchemicals.com
Product Name: R121919|Cas Number: 195055-03-9| Catalog Number: DC10401|Other Nmaes: NBI30775; R 121919; R-121919
R121919 is a potent small-molecule CRF1 receptor antagonist with a Ki of 2 to 5 nM for the CRF1 receptor and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types.
R121919 is a potent small-molecule CRF1 receptor antagonistwith high affinity for the CRF1 receptor (Ki=2–5 nM) and over 1000-fold weaker activity at the CRF2 receptor, CRF-binding protein, or 70 other receptor types[1].R121919 reduces measures of both anxiety and depression in the depressed patients. R121919 dose dependently decreases adrenocorticopin hormone and corticosterone responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively[1]. R121919 reduces levels of anxiety in mice with a steep dose-response curve. Molecules such as GR, MR, BAG-1 and AP-1 have been identified as some of the drug's intracellular targets[2].
Ecteinascidin 770|cas 114899-80-8
Ecteinascidin 770|cas 114899-80-8
DC Chemicals, Website: www.dcchemicals.com
Product Name: Ecteinascidin 770|Cas Number: 114899-80-8| Catalog Number: DC10400|Other Nmaes: Ecteinascidine 770; Et 770; Et-770; Et770
Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.
Ecteinascidin 770 induces apoptosis of U373MG cells. The IC50 concentration of ecteinascidin 770 for killing U373MG glioblastoma cells in culture by using the MTT assay is 4.83 nM by a 72 hour-treatment[1]. The IC50 values against human cell lines HCT116, QG56, and DU145 are 0.6, 2.4, and 0.81 nM, respectively[2]. ET-770 is shown to enhance anoikis response of human lung cancer H23 cells in a dose-dependent manner. Ecteinascidin 770 sensitizes the cells by activating the p53 protein, which in turn down-regulates anti-apoptotic myeloid cell leukemia sequence-1 (MCL1) and up-regulates BCL2-associated X protein (BAX) proteins. However, B-cell lymphoma-2 (BCL2) proteins are not significantly affected by Ecteinascidin 770. The anoikis sensitization of ET-770 is observed in H460 lung cancer cells[3].
DC Chemicals, Website: www.dcchemicals.com
Product Name: Ecteinascidin 770|Cas Number: 114899-80-8| Catalog Number: DC10400|Other Nmaes: Ecteinascidine 770; Et 770; Et-770; Et770
Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.
Ecteinascidin 770 induces apoptosis of U373MG cells. The IC50 concentration of ecteinascidin 770 for killing U373MG glioblastoma cells in culture by using the MTT assay is 4.83 nM by a 72 hour-treatment[1]. The IC50 values against human cell lines HCT116, QG56, and DU145 are 0.6, 2.4, and 0.81 nM, respectively[2]. ET-770 is shown to enhance anoikis response of human lung cancer H23 cells in a dose-dependent manner. Ecteinascidin 770 sensitizes the cells by activating the p53 protein, which in turn down-regulates anti-apoptotic myeloid cell leukemia sequence-1 (MCL1) and up-regulates BCL2-associated X protein (BAX) proteins. However, B-cell lymphoma-2 (BCL2) proteins are not significantly affected by Ecteinascidin 770. The anoikis sensitization of ET-770 is observed in H460 lung cancer cells[3].
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