Aprocitentan

Aprocitentan

CAT N°: 34915
Price:

122.00 103.70

Aprocitentan is a dual endothelin type A (ETA) and ETB receptor antagonist and an active metabolite of macitentan (Item No. 23304).{62420} It is formed from macitentan by the cytochrome P450 (CYP) isoform CYP3A4. Aprocitentan inhibits increases in intracellular calcium induced by endothelin-1 (ET-1) in primary human pulmonary arterial smooth muscle cells (HPASMCs; IC50 = 14 nM), ET-1-induced contractions in isolated rat aortic rings (pA2 = 6.7 for ETA), and sarafotoxin S6c-induced contractions of isolated rat tracheal rings (pKB = 5.5 for ETB).{36210} It reduces ET-1-induced increases in the proliferation of isolated human skin fibroblasts when used at concentrations of 10 and 100 µM.{58774} Aprocitentan (10-300 mg/kg) increases plasma ET-1 concentrations in normotensive rats and decreases mean arterial pressure (MAP) in DOCA-salt hypertensive rats.{58775}

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