SKU : MC536650
CAS Number : 195529-54-5
Molecular Formula : C33H38N2O6 | Molecular Weight : 558.66
Quote RequestPurity | NLT 98% |
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Storage | at 20ºC 2 years |
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Chemical Name | A-192621 |
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CAS Number | 195529-54-5 |
MDL Number | MFCD05662209 |
Molecular Formula | C33H38N2O6 |
Molecular Weight | 558.66 |
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]. In Vitro: 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].
In Vivo: 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].
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