A-804598

N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine
A Potent and Selective Antagonist of P2X7 Receptors
    Cat #: A-415
    Alternative Name N-Cyano-N′′-[(1S)-1-phenylethyl]-N′-5-quinolinyl-guanidine
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 315.37
    Purity: >99%
    Effective concentration 1-100 nM.
    Structure
    • A-804598
    Chemical name 1-cyano-2-[(1S)-1-phenylethyl]-3-quinolin-5-ylguanidine.
    Molecular formula C19H17N5.
    CAS No.: 1125758-85-1.
    PubChem CID 53325874
    Activity A-804598 is a potent and selective, competitive and high-affinity antagonist of the purinergic P2X7 receptor, with IC50 values of around 10 nM for mouse, rat, and human receptors1-3.
    References-Activity
    1. Donnelly-Roberts, D.L. et al. (2009) Neuropharmacology 56, 223.
    2. Able, S.L. et al. (2011) Br. J. Pharmacol. 162, 405.
    3. Bhattacharya, A. et al. (2013) Br. J. Pharmacol. 170, 624.
    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 Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
    Storage of solutions Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • A-804598
      Alomone Labs A-804598 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose-response curve of hP2X7 inhibition by A-804598 (#A-415). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of A-804598, and stimulated with 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 10 nM
    References - Scientific background
    1. Donnelly-Roberts, D.L. et al. (2009) Neuropharmacology 56, 223.
    2. Chizh, B.A. and Illes, P. (2001) Pharmacol. Rev. 53, 553.
    Scientific background

    A-804598 is a potent, competitive, and selective antagonist of the P2X7 receptor. It displays IC50 values of 10 nM, 9 nM and 11 nM for rat, mouse and human P2RX7, respectively1.

    P2X receptors are a family of ligand-gated cation channels activated by the binding of extracellular ATP. To date, seven members of this family have been identified and shown to function as either homomeric or heteromeric combinations2. P2X7 receptors mediate the release of proinflammatory cytokines2.

    Target P2X7 receptors
    Last update: 24/01/2020

    A-804598 (#A-415) is a highly pure, synthetic, and biologically active compound. 

    For research purposes only, not for human use
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