中文名:瑞卢戈利
英文名:Relugolix
纯度:Moligand™,≥98%
货号:R413337
Cas号:737789-87-6
存储温度:-20°C储存
运输条件:超低温运输
产品介绍:
Information
Relugolix Relugolix (RVT-601, TAK-385) is a selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with IC50 of 0.33 nM and 0.32 nM for human GnRHR and monkey GnRHR, respectively.
Targets
monkey GnRHR (Cell-free assay); human GnRHR (Cell-free assay) 0.32 nM; 0.33 nM
In vitro
Relugolix (TAK-385) possesses higher affinity and potent antagonistic activity for human (binding IC50=0.33 nM in the presence of serum) and monkey GnRH receptor (IC50=0.32 nM), but has low affinity for the rat GnRH receptor (IC50=9800 nM).
In vivo
TAK-385 acts as an antagonist for human GnRH receptor in vivo and daily oral administration potently, continuously and reversibly suppresses the hypothalamic-pituitary-gonadal axis.
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