1103522-45-7

N-Despropyl-macitentan, is an active metabolite which is part of a family of endothelin receptor antagonist that allows for treatment of pulmonary arterial hypertension (PAH)

ChEBI: ACT-132577 is a member of the class of sulfamides in which one of the amino groups of sulfonamide is substituted by a 5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl group. An active metabolite of macitentan (obtained by oxidative depropylation), an orphan drug used for the treatment of pulmonary arterial hypertension. It has a role as an antihypertensive agent, an endothelin receptor antagonist, a drug metabolite and a xenobiotic metabolite. It is an aromatic ether, an organobromine compound, a member of pyrimidines and a member of sulfamides. It is functionally related to an ethylene glycol.

ET_A: 3.4 nM (IC₅₀); ET_A: 6.7 (pA2); ET_B: 987 nM (IC₅₀); ET_B: 5.5 (pA2)

Store at -20°C