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Gefapixant citrate

CAS No. 2310299-91-1

Gefapixant citrate( —— )

Catalog No. M35748 CAS No. 2310299-91-1

Gefapixant citrate is an orally active P2X3 receptor (P2X3R) antagonist that acts on human homologous recombinant hP2X3 (IC50: ~30 nM) and hP2X2/3 (IC50: 100-200 nM).

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Gefapixant citrate
  • Note
    Research use only, not for human use.
  • Brief Description
    Gefapixant citrate is an orally active P2X3 receptor (P2X3R) antagonist that acts on human homologous recombinant hP2X3 (IC50: ~30 nM) and hP2X2/3 (IC50: 100-200 nM).
  • Description
    Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis.
  • In Vitro
    Gefapixant citrate displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC50 values >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels).
  • In Vivo
    Gefapixant citrate (7d bid, orally) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses in a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate).
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Others
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2310299-91-1
  • Formula Weight
    545.52
  • Molecular Formula
    C20H27N5O11S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    OC(=O)CC(O)(CC(O)=O)C(O)=O.COc1cc(C(C)C)c(Oc2cnc(N)nc2N)cc1S(N)(=O)=O
  • Chemical Name
    ——

Shipping & Storage Information

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

Reference

1. Anthony P. Ford, et al. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013; 7: 267.?
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