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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

CAS:441798-33-0
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;
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

安全信息

生产方法及用途

合成路线

上游原料

下游产品

图谱

13C NMR : Predict


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