GW 791343 hydrochloride

GW 791343 trihydrochloride, 2-[(3,4-Difluorophenyl)amino]-N-[2-methyl-5-(1-piperazinylmethyl)phenyl]-acetamide trihydrochloride
A Negative Allosteric Modulator of Human P2X7 Receptors
    Cat #: G-115
    Alternative Name GW 791343 trihydrochloride, 2-[(3,4-Difluorophenyl)amino]-N-[2-methyl-5-(1-piperazinylmethyl)phenyl]-acetamide trihydrochloride
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 483.81
    Purity: >99%
    Effective concentration 0.1-10 µM.
    Structure
    • GW 791343 hydrochloride
    Chemical name 2-(3,4-difluoroanilino)-N-[2-methyl-5-(piperazin-1-ylmethyl)phenyl]acetamide trihydrochloride.
    Molecular formula C20H27Cl3F2N4O ( C20H24F2N4O · 3HCl ).
    CAS No.: 309712-55-8, 1019779-04-4.
    PubChem CID 9848159
    Activity GW 791343 hydrochloride is a species-specific allosteric modulator of the purinergic P2X7 receptors, acting as a negative modulator of human P2X7 (pIC50 = 6.9 - 7.2), and as a positive modulator of rat P2X71,2.
    References-Activity
    1. Michel, A.Det al. (2008) Br. J. Pharmacol153, 737.
    2. Michel, A.D. et al. (2008) Br. J. Pharmacol. 155, 738.
    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 and in water. 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
    • GW 791343 hydrochloride
      Alomone Labs GW 791343 hydrochloride inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose response curve of hP2X7 inhibition by GW 791343 hydrochloride (# G-115). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of GW 791343 hydrochloride, and stimulated by 80 µM BzATP. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated as 0.4 µM.
    References - Scientific background
    1. Michel, A.Det al. (2008) Br. J. Pharmacol153, 737.
    2. Michel, A.D. et al. (2008) Br. J. Pharmacol. 155, 738.
    3. Bhattacharya, A. et al. (2013) Br. J. Pharmacol. 170, 624
    4. Swanson, D.M. et al. (2016) J. Med. Chem. 59, 8535.
    Scientific background

    GW 791343 hydrochloride is a species-specific allosteric modulator of purinergic P2X7 receptor. The compound acts as a negative modulator of human P2X7 receptors and as a positive modulator of rat P2X71. GW 791343 displays pIC50 values between 6.9 - 7.2 on human P2X7 receptors1,2.

    P2X receptors are a family of ligand-gated cation channels activated by extracellular ATP, a ligand that mediates numerous cellular and biological functions. Seven members of P2X receptors are identified and shown to function either in homomeric or heteromeric combinations. The P2X receptors are widely localized in cell types of almost every origin, including neuronal, muscular, epithelial and immune and play a pivotal role in models of various pain conditions. P2X7 receptors are responsible for mediating the release of proinflammatory cytokines in inflammatory/immune conditions and pain1,3,4.

    Target P2X7 receptors
    Last update: 24/01/2020

    GW 791343 hydrochloride (#G-115) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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