195529-54-5
195529-54-5 structure
- Name: A-192621
- Chemical Name: (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(2,6-diethylanilino)-2-oxoethyl]-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid
- CAS Number: 195529-54-5
- Molecular Formula: C33H38N2O6
- Molecular Weight: 558.66500
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2017-03-19 15:15:39
- Modify Date: 2024-01-03 16:11:06
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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[1][2][3].
| Name | (2R,3R,4S)-4-(1,3-benzodioxol-5-yl)-1-[2-(2,6-diethylanilino)-2-oxoethyl]-2-(4-propoxyphenyl)pyrrolidine-3-carboxylic acid |
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| Synonyms | (2R,3R,4S)-2-(4-propoxyphenyl)-4-(1,3-benzodioxol-5-yl)-1-(N-[2,6-diethylphenyl]acetamido)pyrrolidine-3-carboxylic acid |
| Description | 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[1][2][3]. |
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| Related Catalog | |
| Target |
ETB:4.5 nM (IC50) ETB:8.8 nM (Ki) ETA:4280 nM (IC50) ETA:5600 nM (Ki) |
| In Vitro | A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner[2]. 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[2]. Cell Viability Assay[2] 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[2] 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. |
| 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 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[3]. Animal Model: Male Sprague-Dawley rats (250-350 g)[3] 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. |
| References |
| Molecular Formula | C33H38N2O6 |
|---|---|
| Molecular Weight | 558.66500 |
| Exact Mass | 558.27300 |
| PSA | 100.82000 |
| LogP | 6.39630 |