A-192621
目录号 : KM11037 CAS No. : 195529-54-5 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg 询价 In-stock
50mg 询价 In-stock

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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.

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.
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.

Cell Viability Assay

Cell Line: Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
Concentration: 1 μM, 10 μM, 50 μM, 100 μM
Incubation Time: 72 hours
Result: The viability of PASMCs was significantly decreased in a dose-dependent manner.

Western Blot Analysis

Cell Line: Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 72 hours
Result: The caspase-3/7 activity in PASMCs was significantly increased in a dose-dependent manner.
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.

Animal Model: Male Sprague-Dawley rats (250-350 g)
Dosage: 30 mg/kg 100 mg/kg
Administration: Oral administration; daily; for 3 days
Result: Inhibited both dilatory and pressor responses induced by S6c mediated by ETB with an ED50value of 30 mg/kg.
分子式
C33H38N2O6
分子量
558.66
CAS号
195529-54-5
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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