Sufugolix

Sufugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 0.1 nM). Sufugolix inhibits GnRH-induced arachidonic acid (Cay-90010, Cay-90010.1, Cay-10006607) release in CHO cells expressing human recombinant or monkey recombinant GnRH (IC50s = 0.1 and 10 nM, respectively), but not the rat GnRH receptor. It inhibits luteinizing hormone (LH) release stimulated by GnRH in monkey pituitary cells ex vivo (IC50 = 36 nM). Sufugolix (10 and 30 mg/kg) reduces increases in plasma LH following castration in male cynomolgus monkeys and lowers serum LH, estradiol, and progesterone levels in female cynomolgus monkeys when administered at a dose of 90 mg/kg.Formal Name: N-[4-[1-[(2,6-difluorophenyl)methyl]-1,2,3,4-tetrahydro-5-[[methyl(phenylmethyl)amino]methyl]-2,4-dioxo-3-phenylthieno[2,3-d]pyrimidin-6-yl]phenyl]-N'-methoxy-urea. CAS Number: 308831-61-0. Synonyms: TAK-013. Molecular Formula: C36H31F2N5O4S. Formula Weight: 667.7. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5mg/mL, DMF:PBS (pH 7.2) (1:2): 0.3mg/mL, DMSO: 3mg/mL. lambdamax: 299 nm. SMILES: O=C1N(C2=CC=CC=C2)C(C(C(CN(C)CC3=CC=CC=C3)=C(C4=CC=C(NC(NOC)=O)C=C4)S5)=C5N1CC6=C(F)C=CC=C6F)=O. InChi Code: InChI=1S/C36H31F2N5O4S/c1-41(20-23-10-5-3-6-11-23)21-28-31-33(44)43(26-12-7-4-8-13-26)36(46)42(22-27-29(37)14-9-15-30(27)38)34(31)48-32(28)24-16-18-25(19-17-24)39-35(45)40-47-2/h3-19H,20-22H2,1-2H3,(H2,39,40,45). InChi Key: UCQSBGOFELXYIN-UHFFFAOYSA-N.