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A-317491 sodium salt hydrate

A Selective Antagonist of P2X3 and P2X2/3 Receptors

Cat #: A-380
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 565.57 (free acid, anhydrous)
    Purity: >98% (HPLC)
    Effective concentration 50 nM – 50 µM.
    Structure
    Chemical name 5-[(3-phenoxyphenyl)methyl-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl]carbamoyl]benzene-1,2,4-tricarboxylic acid.
    Molecular formula C33H27NO8 + xNa + xH2O.
    CAS No.: 475205-49-3
    PubChem CID 9829395
    Activity A-317491 sodium salt hydrate is a selective antagonist of the P2X3 and P2X2/3 receptors. It was shown to inhibit human homomeric P2X3 and heteromeric P2X2/3 receptors with pIC50 values of ~7, whilst exhibiting little to no antagonistic activity on other P2X family receptors, and no effect on P2Y2 at over 10 µM1. This non-nucleotide antagonist reduces chronic inflammatory and neuropathic pain in the rat2.
    References-Activity
    1. Jarvis, M.F. et al. (2002) Proc. Natl. Acad. Sci. U.S.A. 99, 17179.
    2. Donnelly-Roberts, D. et al. (2008) J. Pharmacol. Exp. Ther. 324, 409.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs A-317491 sodium salt hydrate inhibits P2X3 channels expressed in HEK-293 cells.
      Alomone Labs A-317491 sodium salt hydrate inhibits P2X3 channels expressed in HEK-293 cells.
      Dose-response curve of P2X3 inhibition by A-317491 sodium salt hydrate (#A-380). Cells were loaded with Calcium-6 dye, incubated for 5 min with increasing concentrations of A-317491 sodium salt hydrate, and stimulated by 3 µM α,β-MeATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was determined as 7.84 µM.
    References - Scientific background
    1. Jarvis, M.F. et al. (2002) Proc. Natl. Acad. Sci. U.S.A. 99, 17179.
    2. Donnelly-Roberts, D. et al. (2008) J. Pharmacol. Exp. Ther. 324, 409.
    3. Pijacka, W. et al. (2016) Nat. Med. 22, 1151.
    Scientific background

    A-317491 is a selective, competitive, non-nucleotide antagonist of P2X3 and P2X2/3 receptors. It is shown to inhibit human homomeric P2X3 and heteromeric P2X2/3 receptors with pIC50 values of ~7 and exhibits almost no antagonistic activity on other P2X family receptors1. The compound is active in chronic inflammatory and neuropathic pain models, but is ineffective in reducing nociception in animal models of acute, postoperative, and visceral pain.

    A-317491 is the chiral pure S-enantiomer, while the R-enantiomer, A-317344, shows lower activity at P2X3 and P2X2/3 receptors in vitro and lacks anti-nociceptive effects in animal models. A-317491 shows high systemic bioavailability following subcutaneous administration but lacks oral bioavailability. It is not susceptible to metabolic degradation1,2.

    P2X receptors are a family of ion channels gated by ATP. They are expressed in cell types of almost every origin, including neuronal, muscular, epithelial and immune and have been shown to play a pivotal role in models of various pain conditions3.

    Target P2X3 receptors
    Last update: 11/04/2021

    A-317491 sodium salt hydrate (#A-380) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information