Formulation: A solid
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
Purity: ≥98%
Formula Markup: C16H15FN6OS
Formula Weight: 358,4
Shelf life (days): 1460
CAS Number: 1629229-37-3
Notes: Fezolinetant is a neurokinin-3 (NK3) receptor antagonist (IC50 = 20 nM).{66523} 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 (17β-estradiol; Item No. 10006315), follicle-stimulating hormone (FSH), progesterone (Item No. 15876), or testosterone in ovariectomized rats.{66524} 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.
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