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Ro-51

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

Cat #: R-195
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 474.29
    Purity: >98% (HPLC)
    Effective concentration 0.2 nM – 0.2 µM.
    Structure
    Chemical name 2-[[4-amino-5-(5-iodo-4-methoxy-2-propan-2-ylphenoxy)pyrimidin-2-yl]amino]propane-1,3-diol.
    Molecular formula C17H23IN4O4.
    CAS No.: 1050670-85-3
    PubChem CID 24883277
    Activity Ro-51 is a highly potent and selective antagonist of P2X3 and P2X2/3 receptors. It has been shown to inhibit rat homomeric P2X3 and human heteromeric P2X2/3 receptors with pIC50 values of 8.7 and 8.3, respectively, whilst exhibiting no antagonistic activity at other P2X receptor family members at up to 10 µM1.
    References-Activity
    1. Jahangir, A. et al. (2009) Bioorg. Med. Chem. Lett. 19, 1632.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at +4°C for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Up to 100 mM in DMSO or Ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs Ro-51 inhibits P2X3 channels expressed in HEK-293 cells.
      Alomone Labs Ro-51 inhibits P2X3 channels expressed in HEK-293 cells.
      Dose-response curve of P2X3 inhibition by Ro-51 (#R-195). Cells were loaded with Calcium-6 dye, incubated for 5 min with increasing concentrations of Ro-51, 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 at 4 nM.
    References - Scientific background
    1. Jahangir, A. et al. (2009) Bioorg. Med. Chem. Lett. 19, 1632.
    2. Serrano, A. et al. (2012) J. Neurosci. 32, 11890.
    3. Pijacka, W. et al. (2016) Nat Med. 22, 1151.
    Scientific background

    Ro-51 is a highly potent and selective antagonist of P2X3 and P2X2/3 receptors. It inhibits rat homomeric P2X3 and human heteromeric P2X2/3 and demonstrates IC50 values of 2 and 5 nM respectively1.

    Ro-51 has been shown to reduced hyperalgesia and mechanical allodynia in inflammatory and neuropathic pain models1,2. The compound is highly selective for P2X3 and P2X2/3, showing no antagonistic activity at other P2X receptor family members1.

    P2X receptors are a family of ion channels gated by ATP. They 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 conditions3.

    Target P2X3 receptors
    Last update: 12/08/2021

    Ro-51 (#R-195) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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