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JNJ-47965567

JNJ-479655, 2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl-3-pyridinecarboxamide
A Potent and Selective Antagonist of P2X7 Receptors
Cat #: J-115
Alternative Name JNJ-479655, 2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl-3-pyridinecarboxamide
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 488.65
    Purity: >99% (HPLC)
    Effective concentration 20 nM – 1 µM.
    Structure
    Chemical name N-[[4-(4-phenylpiperazin-1-yl)oxan-4-yl]methyl]-2-phenylsulfanylpyridine-3-carboxamide.
    Molecular formula C28H32N4O2S.
    CAS No.: 1428327-31-4.
    PubChem CID 66553218
    Activity JNJ-47965567 is a potent and highly selective antagonist of purinergic P2X7 receptors, shown to inhibit BzATP-induced Ca2+ responses at human, rat and mouse P2X7 receptors with pIC50 values of 8.3, 7.2 and 7.5, respectively. JNJ-47965567 is centrally permeable and active in vivo1.
    References-Activity
    1. 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 +4°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 JNJ-47965567 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs JNJ-47965567 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose response curve of hP2X7 inhibition by JNJ-47965567 (#J-115). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of JNJ-47965567, 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 69 nM.
    References - Scientific background
    1. Bhattacharya, A. et al. (2013) Br. J. Pharmacol. 170, 624.
    2. Swanson, D.M. et al. (2016) J. Med. Chem. 59, 8535.
    Scientific background

    JNJ-47965567 is a synthetic compound that acts as a potent, selective, and high affinity antagonist of P2X7 receptors. It inhibits BzATP-induced Ca2+ responses in human, rat and mouse P2X7 receptors with pIC50 values of 8.3, 7.2 and 7.5, respectively. JNJ-47965567 is centrally permeable and is active in vivo.  The compound can be used as a tool to explore the role of P2X7 in models of CNS pathophysiology.

    Studies show that JNJ-47965567 may attenuate amphetamine induced hyperactivity and exhibits significant efficacy in rat models of neuropathic pain1.

    P2X receptors are detected in neuronal, muscular, epithelial and immune cells and have been shown to 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 pain1,2.

    Target P2X7 receptors
    Last update: 23/08/2020

    JNJ-47965567 (#J-115) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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