macitentan

Macitentan (ACT-064992) 是一种内皮素受体拮抗剂，用于治疗肺动脉高压。

Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.

N-Despropyl Macitentan-d4 是 N-Despropyl Macitentan 的氘代化合物。N-Despropyl Macitentan 的 CAS 号为 1103522-45-7。Aprocitentan 是一种 Macitentan 的主要活性代谢物。它是ETA ETB的双重拮抗剂，其pA2值分别为 6.7 和 5.5，IC50分别为 3.4 nM 和 987 nM。

Macitentan-d4 (ACT-064992 D4) 是一种 Macitentan 氘代物，可被当作非多肽 ETA 和 ETB  (内皮素受体)双拮抗剂。Macitentan-d4 比 Macitentan 毒性更低，半衰期更长，可用于研究由内皮素受体介导介导的疾病。

Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).

ACT-373898 is a metabolite of the endothelin (ET) receptor type A (ETA) and ETBdual antagonist macitentan .1 1.Dingemanse, J., Sidharta, P.N., Maddrey, W.C., et al.Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertensionExpert Opin. Drug Saf.13(3)391-405(2013)

Aprocitentan (ACT-132577) 是一种 Macitentan 的主要活性代谢物。它是 ETA ETB 的双重拮抗剂，其 pA2值分别为 6.7 和 5.5，IC50分别为 3.4 nM 和 987 nM。