Linzagolix

Linzagolix is a nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 36.7 nM for the human receptor). Unlike the peptide GnRH receptor antagonist cetrorelix (Cay-23910), linzagolix (10 µM) does not induce histamine release in isolated rat peritoneal mast cells. Linzagolix (25 and 50 mg/kg) suppresses the menstrual cycle in normal cynomolgus monkeys. It decreases serum luteinizing hormone (LH) levels in ovariectomized cynomolgus monkeys when administered at doses ranging from 1 to 100 mg/kg. Linzagolix (50-200 mg/kg, p.o.) decreases cyst volume in a rat model of endometriosis induced by autotransplantation of endometrial tissue into the renal subcapsular space. Formulations containing linzagolix have been used in the treatment of uterine fibroids.Formal Name: 3-[5-[(2,3-difluoro-6-methoxyphenyl)methoxy]-2-fluoro-4-methoxyphenyl]-1,2,3,4-tetrahydro-2,4-dioxo-thieno[3,4-d]pyrimidine-5-carboxylic acid. CAS Number: 935283-04-8. Synonyms: KLH-2109, OBE-2109. Molecular Formula: C22H15F3N2O7S. Formula Weight: 508.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: O=C(C(SC=C1NC(N2C3=C(F)C=C(OC)C(OCC4=C(C(F)=CC=C4OC)F)=C3)=O)=C1C2=O)O. InChi Code: InChI=1S/C22H15F3N2O7S/c1-32-14-4-3-10(23)18(25)9(14)7-34-16-6-13(11(24)5-15(16)33-2)27-20(28)17-12(26-22(27)31)8-35-19(17)21(29)30/h3-6,8H,7H2,1-2H3,(H,26,31)(H,29,30). InChi Key: BMAAMIIYNNPHAB-UHFFFAOYSA-N.