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Fezolinetant

CAS No. 1629229-37-3

Fezolinetant ( ESN-364;ESN 364 )

Catalog No. M12438 CAS No. 1629229-37-3

A potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Fezolinetant
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6.
  • Description
    A potent, selective, orally active neurokinin-3 receptor (NK3R) antagonist with pIC50/pKi of 7.7/7.6; exhibits high activity in LH inhibition, shows >2.5-log selectivity against NK1R and NK2R subtypes, proves >300-fold selective against related HPG axis receptors (KOR, GnRH, GnIH-R, GPR54).Other Indication Phase 2 Clinical
  • Synonyms
    ESN-364;ESN 364
  • Pathway
    GPCR/G Protein
  • Target
    Neurokinin Receptor
  • Recptor
    Neurokinin Receptor
  • Research Area
    Other Indications
  • Indication
    Other Disease

Chemical Information

  • CAS Number
    1629229-37-3
  • Formula Weight
    358.40
  • Molecular Formula
    C16H15FN6OS
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 50 mg/mL 139.51 mM
  • SMILES
    O=C(C1=CC=C(F)C=C1)N2[C@H](C)C3=NN=C(C4=NC(C)=NS4)N3CC2
  • Chemical 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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Hoveyda HR, et al. ACS Med Chem Lett. 2015 May 19;6(7):736-40.
2. Fraser GL, et al. Endocrinology. 2015 Nov;156(11):4214-25.
3. Fraser GL, et al. J Clin Endocrinol Metab. 2016 Feb;101(2):417-26.
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