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ZINC9315614

ZINC09315614, Z26888283, N-[(2-chloro-6-fluorophenyl)methyl]-N-methyl-5-nitrothiophene-2-carboxamide

An Antagonist of P2X7 Receptors

Cat #: Z-145
Alternative Name ZINC09315614, Z26888283, N-[(2-chloro-6-fluorophenyl)methyl]-N-methyl-5-nitrothiophene-2-carboxamide
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 328.74
    Purity: >98%
    Effective concentration 0.1-10 µM.
    Structure
    Chemical name N-[(2-chloro-6-fluorophenyl)methyl]-N-methyl-5-nitrothiophene-2-carboxamide.
    Molecular formula C13H10ClFN2O3S.
    PubChem CID 17392877
    Activity ZINC9315614 is a novel antagonist of the purinergic P2X7 receptors, shown to inhibit YoPro1 uptake and BzATP-induced Ca2+ responses in HEK–hP2X7 cells with IC50 of 0.8 µM and 3.2 µM, respectively1.
    References-Activity
    1. Caseley, E.A. et al. (2016) Biochem. Pharmacol. 116, 130.
    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 up to 100 mM 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 ZINC9315614 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs ZINC9315614 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose response curve of hP2X7 inhibition by ZINC9315614 (#Z-145). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of ZINC9315614, 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 355 nM.
    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.
    Scientific background

    ZINC9315614 is a selective antagonist of purinergic P2X7 receptors. It binds to the ATP-binding pocket of P2X71. ZINC9315614 inhibits YoPro1 dye uptake and BzATP-induced Ca2+ responses in HEK–human P2X7 cells with IC50 value of 0.8 µM and 3.2 µM, respectively1.

    P2X receptors are cationic trimeric channel complexes that function as ATP-gated calcium-permeable and are considered to be an attractive therapeutic target. This family contains seven receptor subtypes: P2X1–P2X7. P2X7 receptors participate in various cellular responses such as membrane permeabilization, activation of caspases, cytokine release, cell proliferation, and apoptosis. P2X7 receptors can be found in almost all tissues1,2.

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

    ZINC9315614 (#Z-145) 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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