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JNJ 16259685

A Potent and Selective Antagonist of mGluR1

Cat #: J-110
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 325.41
    Purity: >97%
    Effective concentration 1 nM – 1 µM.
    Structure
    Chemical name 3,4-dihydro-2H-pyrano[2,3-b]quinolin-7-yl-(4-methoxycyclohexyl)methanone.
    Molecular formula C20H23NO3.
    CAS No.: 409345-29-5
    PubChem CID 11313361
    Activity JNJ 16259685 is a potent and selective non-competitive antagonist of mGluR1 receptors, inhibiting human mGluR1 and mGluR5 mediated glutamate-induced Ca2+ mobilization with IC50 values of 1.21 nM and 28.3 µM, respectively, whilst having no effect on a range of other receptor subtypes at over 10 µM1.
    It is systemically active, occupying central mGluR1 receptors in the rat cerebellum and thalamus (ED50 = 40 and 14 µg/kg, respectively) when administered subcutaneously1. JNJ 16259685 inhibits synaptic activation of mGluR1 in Purkinje cells in cerebellar slices with IC50 of 19 nM2.
    References-Activity
    1. Lavreysen, H. et al. (2004) Neuropharmacology 47, 961.
    2. Fukunaga, I. et al. (2007) Br. J. Pharmacol. 151, 870.
    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 product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs JNJ 16259685 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs JNJ 16259685 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells.
      Dose-response of JNJ 16259685 (#J-110) normalized inhibition of human mGluR1-mediated, L-Glutamate-evoked Ca2+ mobilization.
      Cells were loaded with a calcium-sensitive dye, incubated with a range of JNJ 16259685 concentrations, and stimulated with 5 µM L-Glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
    References - Scientific background
    1. Fukunaga, I. et al. (2007) Br. J. Pharmacol. 151, 870.
    2. Zheng, G.Z. et al. (2005) J. Med. Chem. 48, 7374.
    Scientific background

    JNJ 16259685 is a potent, specific, and non-competitive antagonist of mGluR1 displaying an IC50 of 19 nM1. The compound shows a much lower potency towards mGluR5 receptor1,2.

    Glutamate is the most abundant excitatory neurotransmitter in the central nervous system and it modulates activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs). mGluRs consist of three groups: I, II, and III with a total of eight subtypes, mGluR1 to mGluR8.

    mGluR1 plays an important role in the central sensitization of pain and in various physiological functions including regulating ion channels, synaptic transmission, and synaptic plasticity2.

    Target mGluR1
    Last update: 11/04/2021

    JNJ 16259685 (#J-110) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information