基本属性 生物活性靶点体外研究体内研究 用途与合成方法 A192621 价格(试剂级) 供应商 供应信息

A192621

A192621

中文名称:A192621
英文名称:A192621
CAS号:195529-54-5
分子式:C33H38N2O6
分子量:558.66
EINECS号:
Mol文件:195529-54-5.mol
A192621 结构式

A192621 性质

沸点 738.3±60.0 °C(Predicted)
密度 1.233±0.06 g/cm3(Predicted)
储存条件 -20°C
形态 粉末
酸度系数(pKa) 3.52±0.60(Predicted)
颜色 白色至米色

A192621 用途与合成方法

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。

ET B

4.5 nM (IC 50 )

ET B

8.8 nM (Ki)

ET A

4280 nM (IC 50 )

ET A

5600 nM (Ki)

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.

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 ED 50 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 ED 50 value of 30 mg/kg.

A192621 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-01-25 HY-120295 A192621 195529-54-5 5mg 2900
2024-01-25 HY-120295 10 mM * 1 mLin DMSO 3564

A192621供应商 更多

北京普西唐生物科技有限公司
联系电话:010-60605840 18892239720
产品介绍:
英文名称:A-192621
CAS:195529-54-5
纯度:98%
包装信息:5mg
ChemeGen 中国
联系电话: 18818260767
产品介绍:
英文名称:A-192621
CAS:195529-54-5
纯度:98%
包装信息:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
备注:品牌:ChemeGen
安耐吉化学&3A(安徽泽升科技有限公司)
联系电话:021-58432009 400-005-6266
产品介绍:
英文名称:A192621 >=98 (HPLC)
CAS:195529-54-5
纯度:NULL
包装信息:1ea;25mg;5mg
备注:NULL
天津普西唐生物医药科技有限公司
联系电话:010-60605840 15801484223
产品介绍:
英文名称:A-192621
CAS:195529-54-5
纯度:98%
包装信息:5mg
北京百奥创新科技有限公司
联系电话: 15522676233
产品介绍:
英文名称:A-192621
CAS:195529-54-5
纯度:>98%
包装信息:5mg;25mg

最新发布供应信息

195529-54-5A-192621
上海一研生物科技有限公司 2024-04-26
A-192621
北京百奥创新科技有限公司 2023-03-10