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化合物简介

Sufugolix (INN, BAN) (developmental code name TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively). It was under development by Takeda for the treatment of endometriosis and uterine leiomyoma and reached phase II clinical trials for both of these indications, but was subsequently discontinued. It seems to have been supplanted by relugolix (TAK-385), which is also under development by Takeda for the treatment of these conditions and has a more favorable drug profile (including reduced cytochrome P450 inhibition and improved in vivo GnRHR antagonistic activity) in comparison.

基本信息

CAS:308831-61-0
中文别名
英文别名
分子式:C36H31F2N5O4S
分子量:667.724
精确质量:667.206
Psa:125.84
Logp:6.9862

编号系统

物化性质

密度:1.383g/cm3
折射率:1.667

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

1H NMR : Predict


13C NMR : Predict


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