An NK3 receptor antagonist
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Fezolinetant

Item No. 39523

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A solid
Solubility(Learn about Variance in 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $112

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    10 mg

    $212

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    25 mg

    $501

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    50 mg

    $945

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    Product Description

    Fezolinetant is a neurokinin-3 (NK3) receptor antagonist (IC50 = 20 nM).1 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.2 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hoveyda, H.R., Fraser, G.L., Dutheuil, G., et al. Optimization of novel antagonists to the neurokinin-3 receptor for the treatment of sex-hormone disorders (Part II). ACS Med. Chem. Lett. 6(7), 736-740 (2015).

    2. Tahara, A., Takamatsu, H., Ohtake, A., et al. Effects of neurokinin 3 receptor antagonist fezolinetant on hot flash-like symptoms in ovariectomized rats. Eur. J. Pharmacol. 905, 174207 (2021).