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A Potent and Selective Antagonist of P2X3 and P2X2/3 Receptors

Cat #: R-190
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 302.37
    Purity: >97% (HPLC)
    Effective concentration 50 nM – 50 µM.
    Chemical name 5-[(4,5-dimethoxy-2-propan-2-ylphenyl)methyl]pyrimidine-2,4-diamine.
    Molecular formula C16H22N4O2.
    CAS No.: 1026582-88-6
    PubChem CID 11289644
    Activity RO-3 is a potent and selective antagonist of the P2X3 and P2X2/3 receptors. It inhibits human homomeric P2X3 and heteromeric P2X2/3 receptors with pIC50 values of 7.0 and 5.9, respectively, whilst showing selectivity over other homomeric P2X family receptors with pIC50 of < 51.
    1. Ford, A. et al. (2006) Br. J. Pharmacol. 147, S132.
    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 RO-3 inhibits P2X3 channels expressed in HEK-293 cells.
      Alomone Labs RO-3 inhibits P2X3 channels expressed in HEK-293 cells.
      Dose-response curve of P2X3 inhibition by RO-3 (#R-190). hP2X3/HEK-293 cells were loaded with Calcium-6 dye, incubated for 5 min with rising concentrations of RO-3, 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 1.11 µM.
    References - Scientific background
    1. Ford, A. et al. (2006) Br. J. Pharmacol. 147, S132.
    2. Pijacka, W. et al. (2016) Nat. Med. 22, 1151.
    Scientific background

    RO-3 is a potent inhibitor of human homomultimeric P2X3 receptor and heteromultimeric P2X2/3 receptor and demonstrates pIC50 value of 7.0 and pIC50=5.9 respectively1.

    The compound shows to have to high metabolic stability in rat and human hepatocytes and liver microsomes. It's highly permeable, orally bioavailable, and has a good in vivo plasma half-life in rats. RO-3 is also widely distributed to tissues after administration, with low plasma protein binding and good CNS penetration1.

    The P2X receptors are a family of ion channels that are gated by ATP. P2X receptors are widely localized 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 conditions2.

    Target P2X3 receptors
    Last update: 06/11/2022

    RO-3 (#R-190) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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