TAK-385

A GnRH receptor antagonist

TAK-385 is an orally bioavailable gonadotropin-releasing hormone receptor (GnRHR) antagonist (IC50s = 0.33 and 0.32 nM for the human and monkey receptors, respectively).1 It is selective for these receptors over the rat GnRHR receptor (IC50 = 9,800 nM), as well as a panel of 134 enzymes and receptors at 10 µM. TAK-385 is 95-fold more potent at inhibiting GnRH-induced arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) release in CHO cells expressing human GnRHR compared with those expressing monkey GnRHR. It decreases testis, ventral prostate, ovary, and uterus weight in human GNRHR knock-in mice when administered at doses ranging from 3 to 200 mg/kg per day for 28 days.2 TAK-385 (1 and 3 mg/kg) also decreases plasma luteinizing hormone levels in castrated cynomolgus monkeys.1

623.6

≥98%

Relugolix

CN(C)CC1=C(C2=CC=C(NC(NOC)=O)C=C2)SC3=C1C(N(C4=CC=C(OC)N=N4)C(N3CC5=C(F)C=CC=C5F)=O)=O

C29H27F2N7O5S

737789-87-6

≥ 4 years

DMF: 25 mg/ml DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml DMSO: 20 mg/ml Ethanol: 1 mg/ml