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A-839977

1-(2,3-Dichlorophenyl)-N-[2-(pyridin-2-yloxy)benzyl]-1H-tetrazol-5-amine

A Potent and Selective Antagonist of P2X7 Receptors

Cat #: A-470
Alternative Name 1-(2,3-Dichlorophenyl)-N-[2-(pyridin-2-yloxy)benzyl]-1H-tetrazol-5-amine
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 413.26
    Purity: >96%
    Effective concentration 1-50 nM.
    Structure
    Chemical name 1-(2,3-dichlorophenyl)-N-[(2-pyridin-2-yloxyphenyl)methyl]tetrazol-5-amine.
    Molecular formula C19H14Cl2N6O.
    CAS No.: 870061-27-1
    PubChem CID 53325875
    Activity A-839977 is a potent and selective antagonist of P2X7 receptors, shown to inhibit BzATP-induced Ca2+ responses at human, rat and mouse P2X7 receptors with IC50 values of 20 nM, 42 nM and 150 nM, respectively. A-839977 produces significant anti-nociception and anti-hyperalgesia (ED50 = 40-100μmol/kg) in animal models of inflammatory pain1.
    References-Activity
    1. Honore, P. et al. (2009) Behav. Brain. Res. 204, 77.
    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 -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
    Our bioassay
    • Alomone Labs A-839977 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs A-839977 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose-response curve of hP2X7 inhibition by A-839977 (#A-470). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of A-839977, 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 8 nM
    References - Scientific background
    1. Honore, P. et al. (2009) Behav. Brain. Res. 204, 77.
    2. Stokes, L. et al. (2006) Br. J. Pharmacol. 149, 880.
    3. Donnelly-Roberts, D.L. et al. (2009) Br. J. Pharmacol. 157, 1203.
    Scientific background

    A-839977 is a potent and selective antagonist of the P2X7 receptor. It inhibits BzATP-induced Ca2+ responses of human, rat and mouse P2X7 receptors with IC50 values of 20 nM, 42 nM and 150 nM, respectively1.

    Selective P2X7 receptor antagonists, including A-839977, reduce inflammatory and neuropathic pain in animal models. In mice, A-839977 produces robust anti-hyperalgesia in a model of inflammatory pain.

    The P2X7 receptor is a member of the ligand-gated ion channels activated by extracellular ATP. There are seven receptor subtypes: P2X1–P2X7. P2X7 receptors participate in a variety of cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. P2X7 receptors are highly expressed throughout autonomic, sensory and central neurons and in visceral smooth muscle, immune cells and epithelia2,3.

    Target P2X7 receptors
    Lyophilized Powder
    Last update: 06/11/2022

    A-839977 (#A-470) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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