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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 |
| 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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