A192621
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- CAS号:
- 195529-54-5
- 英文名:
- A192621
- 英文别名:
- A192621;A192621,CID 5310991;A192621 >=98 (HPLC);(2R,3R,4S)-4-(1,3-BENZODIOXOL-5-YL)-1-[2-[(2,6-DIETHYLPHENYL)AMINO]-2-OXOETHYL]-2-(4-PROPOXYPHENYL)PYRROLIDINE-3-CARBOXYLIC ACID;3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-, (2R,3R,4S)-
- 中文名:
- A192621
- 中文别名:
- 化合物 T14068
- CBNumber:
- CB23369698
- 分子式:
- C33H38N2O6
- 分子量:
- 558.66
- MOL File:
- 195529-54-5.mol
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A192621化学性质
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沸点:
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738.3±60.0 °C(Predicted)
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密度:
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1.233±0.06 g/cm3(Predicted)
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储存条件:
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-20°C
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形态:
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powder
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酸度系数(pKa):
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3.52±0.60(Predicted)
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颜色:
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white to beige
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A192621性质、用途与生产工艺
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。
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ET
B
4.5 nM (IC
50
)
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ET
B
8.8 nM (Ki)
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ET
A
4280 nM (IC
50
)
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ET
A
5600 nM (Ki)
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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
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Cell Line:
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Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
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Concentration:
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1 μM, 10 μM, 50 μM, 100 μM
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Incubation Time:
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72 hours
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Result:
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The viability of PASMCs was significantly decreased in a dose-dependent manner.
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Western Blot Analysis
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Cell Line:
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Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
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Concentration:
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1 μM, 10 μM, 100 μM
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Incubation Time:
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72 hours
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Result:
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The caspase-3/7 activity in PASMCs was significantly increased in a dose-dependent manner.
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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.
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Animal Model:
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Male Sprague-Dawley rats (250-350 g)
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Dosage:
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30 mg/kg 100 mg/kg
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Administration:
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Oral administration; daily; for 3 days
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Result:
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Inhibited both dilatory and pressor responses induced by S6c mediated by ET
B
with an ED
50
value of 30 mg/kg.
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A192621
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上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-120295 | A192621
A-192621 | 195529-54-5 | 5mg | 2900元 |
| 2024/01/25 | HY-120295 | A-192621 | | 10 mM * 1 mLin DMSO | 3564元 |
195529-54-5, A192621 相关搜索:
- 抑制剂
- 制剂-拮抗剂
- 化合物 T14068
- 195529-54-5
- A192621 >=98 (HPLC)
- 3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-[2-[(2,6-diethylphenyl)amino]-2-oxoethyl]-2-(4-propoxyphenyl)-, (2R,3R,4S)-
- A192621,CID 5310991
- A192621
- (2R,3R,4S)-4-(1,3-BENZODIOXOL-5-YL)-1-[2-[(2,6-DIETHYLPHENYL)AMINO]-2-OXOETHYL]-2-(4-PROPOXYPHENYL)PYRROLIDINE-3-CARBOXYLIC ACID