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
Size Price / USD Stock Quantity
5MG 55 In Stock
50MG 221 In Stock
100MG 398 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

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.?
molnova catalog
related products
  • MMP-8 Substrate, flu...

    MMP-8/MMP-26 Fluorogenic substrate (DNP-Pro-Leu-Ala-Tyr-Trp-Ala-Arg) is a matrix metalloproteinase-8 (MMP-8) fluorogenic substrate. MMP-8/MMP-26 Fluorogenic substrate can be used for the research of atherosclerosis, pulmonary fibrosis, and sepsis.

  • CALP1

    Cell-permeable calmodulin (CaM) agonist that binds to the EF-hand/Ca2+-binding site; produces CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites on other Ca2+ channels, including NMDA and HIV-1 gp120-activated channels, inhibiting Ca2+-mediated cytotoxicity and apoptosis (IC50 = 52 μM). Shown to protect pancreatic acinar cells from gossypol induced necrosis. Inhibits VLA-5-mediated adhesion of mast cells to fibronectin in vitro and attenuates inflammatory cell influx in guinea pig lung in vivo.

  • Delta 5-avenasterol

    Delta 5-avenasterol has antioxidant activity.