Formulation: A solid
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
Purity: ≥98%
Formula Markup: C22H15F3N2O7S
Formula Weight: 508,4
Shelf life (days): 1460
CAS Number: 935283-04-8
Notes: Linzagolix is a nonpeptide gonadotropin-releasing hormone (GnRH) receptor antagonist (IC50 = 36.7 nM for the human receptor).{65962} Unlike the peptide GnRH receptor antagonist cetrorelix (Item No. 23910), linzagolix (10 µM) does not induce histamine release in isolated rat peritoneal mast cells.{65963} Linzagolix (25 and 50 mg/kg) suppresses the menstrual cycle in normal cynomolgus monkeys.{65962} 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.{65963} Formulations containing linzagolix have been used in the treatment of uterine fibroids.
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