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 4.5 nM，Ki 为 8.8 nM。A-192621 的选择性比 ETA 高 636 倍 (IC50 为 4280 nM，Ki 为 5600 nM)。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。
| 生物活性 |
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. |
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| 体外研究 |
A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner. Cell Viability Assay
Western Blot Analysis
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| 体内研究 |
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.
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| 分子式 |
C33H38N2O6
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| 分子量 |
558.66
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| CAS号 |
195529-54-5
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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纯度： 98%
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Data Sheet
