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Description | 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. A-192621 promotes apoptosis in PASMCs and elevates both arterial blood pressure and plasma ET-1 levels[1][2][3]. Its selectivity is 636-fold higher for ETB than ETA (IC50 of 4280 nM and Ki of 5600 nM). |
Targets&IC50 | ETB:8.8 nM (ki), ETA:4280 nM, ETA:5600 nM (ki), ETB:4.5 nM |
In vitro | A-192621 induces apoptosis in a dose-dependent manner and increases the cells' susceptibility to apoptosis by Doxorubicin treatment[2]. A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner[2] and it treatment significantly increases the caspase-3/7 activity and cleaved caspase-3 expression in PASMCs. |
In vivo | A-192621 (30-100 mg/kg; oral administration; daily; for 3 days; male Sprague-Dawley rats) inhibits dilatory and pressor responses induced by S6c mediated by ETB, with an ED50 of 30 mg/kg, but fails to inhibit the ET-1-induced pressor response mediated by ETA. A-192621 alone raises arterial blood pressure and plasma ET-1 levels in the conscious normotensive rat[3]. |
Molecular Weight | 558.66 |
Formula | C33H38N2O6 |
Cas No. | 195529-54-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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