Fezolinetant

Fezolinetant is a neurokinin-3 (NK3) receptor antagonist (IC50 = 20 nM). It decreases plasma levels of luteinizing hormone (LH) in castrated cynomolgus monkeys when administered at a dose of 5 mg/kg. Fezolinetant (10 mg/kg) prevents increases in body weight and food intake but does not affect uterine weight or plasma levels of estradiol (17beta-estradiol, Cay-10006315), follicle-stimulating hormone (FSH), progesterone (Cay-15876), or testosterone in ovariectomized rats. It inhibits increases in skin temperature but not core temperature, indicating regulation of hot flash-like symptoms, in ovariectomized rats when administered at doses of 3 or 10 mg/kg. Formulations containing fezolinetant have been used in the treatment of moderate to severe vasomotor symptoms due to menopause.Formal Name: [(8R)-5,6-dihydro-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl](4-fluorophenyl)-methanone. CAS Number: 1629229-37-3. Synonyms: AS 3472693-00, ESN364. Molecular Formula: C16H15FN6OS. Formula Weight: 358.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: C[C@@H]1C2=NN=C(C3=NC(C)=NS3)N2CCN1C(C4=CC=C(C=C4)F)=O. InChi Code: InChI=1S/C16H15FN6OS/c1-9-13-19-20-14(15-18-10(2)21-25-15)23(13)8-7-22(9)16(24)11-3-5-12(17)6-4-11/h3-6,9H,7-8H2,1-2H3/t9-/m1/s1. InChi Key: PPSNFPASKFYPMN-SECBINFHSA-N.