A-192621 - CAS:195529-54-5

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A-192621

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

Data Sheet SDS 产品使用指南

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。

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生物活性

A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ET_B) receptor antagonist with an IC₅₀ of 4.5 nM and a K_i of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ET_A (IC₅₀ of 4280 nM and K_i 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.

IC₅₀&Target

ET_B

4.5 nM (IC₅₀)

ET_B

8.8 nM (Ki)

ET_A

4280 nM (IC₅₀)

ET_A

5600 nM (Ki)

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 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.

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 ET_B 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

纯度： 98%

Data Sheet

SDS

产品使用指南

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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The molarity calculator equation

The dilution calculator equation

动物实验计算换算器