ZINC58368839

N-cycloheptyl-N-methyl-2-(5-nitro-1H-indol-1-yl)acetamide, T6869826, Z905437510
An Antagonist of P2X7 Receptors
    Cat #: Z-135
    Alternative Name N-cycloheptyl-N-methyl-2-(5-nitro-1H-indol-1-yl)acetamide, T6869826, Z905437510
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 329.39
    Purity: >97%
    Effective concentration 5-50 µM.
      • ZINC58368839
    Chemical name N-cycloheptyl-N-methyl-2-(5-nitroindol-1-yl)acetamide.
    Molecular formula C18H23N3O3.
    PubChem CID 51127177
    Activity ZINC58368839 is a novel antagonist of purinergic P2X7 receptors, shown to inhibit BzATP-induced Ca2+ responses in HEK–hP2X7 cells with IC50 of 4.8 µM1.
    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.
      • ZINC58368839
        Alomone Labs ZINC58368839 inhibits human P2X7 receptors expressed in HEK-293 cells.
        Dose response curve of hP2X7 inhibition by ZINC58368839 (#Z-135). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of ZINC58368839, 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 13 µM.
    References - Scientific background
    • 1. Caseley, E.A. et al. (2016) Biochem. Pharmacol. 116, 130.
    • 2. Stokes, L. et al. (2006) Br. J. Pharmacol. 149, 880.
      • ZINC58368839 inhibits P2X7 receptors by binding to the ATP-binding pocket of the receptor and demonstrates strong specificity towards human P2X7R over human P2X4R and rat P2X3R1. It inhibits BzATP-induced Ca2+ responses in HEK–hP2X7 cells with IC50 value of 4.8 µM1.

        P2X receptors are cationic trimeric channel complexes that function as ATP-gated Ca2+-permeable channels. They are considered to be an attractive therapeutic target. This family includes 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 ubiquitously expressed, and particularly in cells of haematopoietic origin1,2.

    Target P2X7 channels
    Last update: 18/07/2019

    ZINC58368839 (#Z-135) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use