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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.
| Molecular Weight | 558.66 |
| Formula | C33H38N2O6 |
| CAS Number | 195529-54-5 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Endothelin Receptor Products |
|---|
| Zibotentan
Zibotentan (ZD4054) is a more selective and specific endothelin-A receptor (ETAR) antagonist with an IC50 value of 21 nM. |
| Ambrisentan
Ambrisentan is an orally active, highly selective antagonist of the endothelin-1 type A receptor. |
| Sitaxsentan sodium
Sitaxsentan (TBC-11251) is an orally active, highly selective antagonist of endothelin A receptors. |
| Macitentan
Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist. |
| Bosentan Hydrate
Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
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