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A-192621

CAS No. : 195529-54-5

MCE 国际站：A-192621

产品活性：A-192621 是一种有效的非肽，口服活性，选择性内皮素 B (ET_B) 受体拮抗剂，IC₅₀ 为 4.5 nM，K_i 为 8.8 nM。A-192621 的选择性比 ET_A 高 636 倍 (IC₅₀ 为 4280 nM，K_i 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。

研究领域：GPCR/G Protein  |  Apoptosis

作用靶点：Endothelin Receptor  |  Apoptosis

In Vitro: A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner.
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.

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 ET_B with an ED₅₀ value of 30 mg/kg, and failed to inhibit the ET-1-induced pressor response mediated by ET_A. 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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