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Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan (ACT-132577) achieves full inhibition of intracellular calcium increase induced by ET-1 on nonrecombinant cells.
| Molecular Weight | 546.19 |
| Formula | C16H14Br2N6O4S |
| CAS Number | 1103522-45-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 23 mg/mL |
| Storage | 2-8°C, protect from light |
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