A-192621
目录号 : GC60544
A-192621是一种有效的非肽,口服活性,选择性内皮素B(ETB)受体拮抗剂,IC50为4.5nM,Ki为8.8nM。A-192621的选择性比ETA高636倍(IC50为4280nM,Ki为5600nM)。A-192621促进PASMC细胞凋亡,并引起动脉血压升高和血浆ET-1水平升高。
Cas No.:195529-54-5
Sample solution is provided at 25 µL, 10mM.
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level[1][2][3].
A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner[2].A-192621 (1-100 μM; 48 hours; PASMCs) treatment significantly increases the caspase-3/7 activity and cleaved caspase-3 expression in PASMCs. A-192621 induces apoptosis in a dose-dependent manner and increases the cells' susceptibility to apoptosis by Doxorubicin treatment[2]. Cell Viability Assay[2] Cell Line: Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
A-192621 (30-100 mg/kg; oral administration; daily; for 3 days; male Sprague-Dawley rats) treatment inhibits both dilatory and pressor responses induced by S6c mediated by ETB with an ED50 value of 30 mg/kg, and failed to inhibit the ET-1-induced pressor response mediated by ETA. A-192621 alone causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level in the conscious normotensive rat[3]. Animal Model: Male Sprague-Dawley rats (250-350 g)[3]
[1]. Wu-Wong JR, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S. [2]. Sakai S, et al. Antagonists to endothelin receptor type B promote apoptosis in human pulmonary arterial smooth muscle cells. Life Sci. 2016 Aug 15;159:116-120. [3]. Wessale JL, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S.
Cas No. | 195529-54-5 | SDF | |
Canonical SMILES | O=C([C@H]1[C@H](C2=CC=C(OCCC)C=C2)N(CC(NC3=C(CC)C=CC=C3CC)=O)C[C@@H]1C4=CC=C(OCO5)C5=C4)O | ||
分子式 | C33H38N2O6 | 分子量 | 558.66 |
溶解度 | DMSO : ≥ 100 mg/mL (179.00 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 1.79 mL | 8.95 mL | 17.9 mL |
5 mM | 0.358 mL | 1.79 mL | 3.58 mL |
10 mM | 0.179 mL | 0.895 mL | 1.79 mL |
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