For research use only. Not Intended for Therapeutic Use!
|Target:||endothelin receptor antagonist|
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ACT-132577 is the major and pharmacologically active metabolite of macitentan(ACT-064992), which is dual ETA/ETB endothelin (ET) receptor antagonist designed for tissue targeting.
Tareget: ETA/ETA receptor
In vivo, macitentan is metabolized into a major and pharmacologically active metabolite, ACT-132577. Macitentan and its metabolite antagonized the specific binding of ET-1 on membranes of cells overexpressing ET(A) and ET(B) receptors and blunted ET-1-induced calcium mobilization in various natural cell lines, with inhibitory constants within the nanomolar range. In functional assays, macitentan and ACT-132577 inhibited ET-1-induced contractions in isolated endothelium-denuded rat aorta (ET(A) receptors) and sarafotoxin S6c-induced contractions in isolated rat trachea (ET(B) receptors). In rats with pulmonary hypertension, macitentan prevented both the increase of pulmonary pressure and the right ventricle hypertrophy, and it markedly improved survival . In both ethnic groups, females had an approximately 15% higher exposure to ACT-132577 than male subjects . ACT-132577, a metabolite with lower potency than macitentan, had a half-life of about 48hours and accumulated approximately 8.5-fold .