化合物简介
Macitentan (trade name Opsumit) is an endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH). The other two ERAs marketed as of 2014 are bosentan and ambrisentan. Macitentan is a dual ERA, meaning that it acts as an antagonist of two endothelin (ET) receptor subtypes, ETA and ETB. However, macitentan has a 50-fold increased selectivity for the ETA subtype compared to the ETB subtype. The drug received approval from the U.S. Food and Drug Administration (FDA) on October 13, 2013.
基本信息
中文名称
马西替坦
英文名称
macitentan
中文别名
N-[5-(4-溴苯基)-6-[2-[(5-溴-2-嘧啶基)氧]乙氧基]-4-嘧啶基]-N\'-丙基磺酰胺
英文别名
Macitentan、5-(4-bromophenyl)-6-[2-(5-bromopyrimidin-2-yl)oxyethoxy]-N-(propylsulfamoyl)pyrimidin-4-amine、Actelion-1、Opsumit
CAS号
441798-33-0
分子式
C19H22Br2N6O4S
分子量
590.289
精确质量
587.979
PSA
159.84
LOGP
5.3724
编号系统
MDL号
MFCD17167076
物化性质
密度
1.675
沸点
692.397ºC at 760 mmHg
闪点
372.548ºC