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JNJ-54166060

(R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridine-5(4H)‑yl)methanone

A Novel Potent and Selective Antagonist of P2X7 Receptors

Cat #: J-125
Alternative Name (R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridine-5(4H)‑yl)methanone
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 438.81
    Purity: >99% (HPLC)
    Effective concentration 10 nM – 1 µM.
    Structure
    Chemical name (R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridine-5(4H)‑yl)methanone.
    Molecular formula C20F4H15N4OCl.
    Activity JNJ-54166060 is a novel, potent and selective antagonist of purinergic P2X7 receptors, with IC50 of 4 nM on human receptors. Orally bioavailable, with an ED50 of 2.3 mg/kg and a brain/plasma ratio of close to 3 in rats1.
    References-Activity
    1. Swanson, D.M. et al. (2016) J. Med. Chem. 59, 8535.
    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 JNJ-54166060 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Alomone Labs JNJ-54166060 inhibits human P2X7 receptors expressed in HEK-293 cells.
      Dose response curve of hP2X7 inhibition by JNJ-54166060 (#J-125). Cells were loaded with Fluo-8 NW dye, incubated with increasing concentrations of JNJ-54166060, 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 65.6 nM.
    References - Scientific background
    1. Swanson, D.M. et al. (2016) J. Med. Chem. 59, 8535.
    2. Broom, D.C. et al. (2008) J. Pharmacol. Exp. Ther. 327, 620.
    3. Pijacka, W. et al. (2016) Nat. Med. 22, 1151.
    Scientific background

    JNJ-54166060 is a potent and selective antagonist of P2X7 receptors, displaying IC50 values of 4 nM for human P2X71. JNJ-54166060 has a high oral bioavailability with low-moderate clearance in preclinical species, and acceptable safety margins in rats1.

    P2X receptors are a family of ion channels gated by ATP, a ubiquitous energy donor and receptor ligand in living cells. P2X receptors are ubiquitously expressed, including expression in neuronal, muscular, epithelial and immune cells and play a pivotal role in models of various pain conditions. P2X7 is responsible for mediating the release of proinflammatory cytokines known to have roles in inflammatory/immune conditions and pain2,3.

    Target P2X7 receptors
    Lyophilized Powder
    Last update: 11/04/2021

    JNJ-54166060 (#J-125) 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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