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A Potent and Selective Antagonist of P2X3 Receptor

Cat #: A-375
Alternative Name RO-4
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 400.21
    Purity: >95% (HPLC)
    Effective concentration 1 nM – 10 µM.
    Chemical name 5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidine-2,4-diamine.
    Molecular formula C14H17IN4O2.
    CAS No.: 865305-30-2
    PubChem CID 15953802
    Activity AF-353 is a highly potent and selective P2X3 and P2X2/3 receptor antagonist. pIC50 for these receptors, measured using intracellular calcium assays and whole-cell voltage-clamp, range from 7.4 to 8.51.
    1. Gever, J.R. et al. (2010) Br. J. Pharmacol. 160, 1387.
    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 25mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs AF-353 inhibits P2X3 receptors expressed in HEK-293 cells.
      Alomone Labs AF-353 inhibits P2X3 receptors expressed in HEK-293 cells.
      Dose-response curve of P2X3 inhibition by AF-353 (#A-375). Cells were loaded with Calcium-6 dye, incubated for 5 min with increasing concentrations of AF-353, 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 9.84 nM.
    References - Scientific background
    1. Gever, J.R. et al. (2010) Br. J. Pharmacol. 160, 1387.
    2. Pijacka, W. et al. (2016) Nat. Med. 22, 1151.
    Scientific background

    AF-353 is a highly potent and selective antagonist of P2X3 and P2X2/3 purinergic receptors. The compound is orally bioavailable and is being used as an in vivo tool for studying the role of P2X channels in animal pain models.

    P2X receptors are a family of ion channels that are 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 conditions1.

    Antagonism of P2X3 receptors can reduce arterial pressure and basal sympathetic activity and normalizes carotid body hyper-reflexia in rats with hypertension2.

    Target P2X3 receptors
    Last update: 06/11/2022

    AF-353 (#A-375) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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