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GTPL1390, SCHEMBL6952709

A Potent and Selective Antagonist of Rat mGluR1 Receptors

Cat #: E-165
Alternative Name GTPL1390, SCHEMBL6952709
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 308.39
    Purity: >98%
    Effective concentration 10 nM – 10 µM.
    Chemical name 1-ethyl-2-methyl-6-oxo-4-(1,2,4,5-tetrahydro-3-benzazepin-3-yl)pyrimidine-5-carbonitrile.
    Molecular formula C18H20N4O.
    PubChem CID 9904703
    Activity EM-TBPC is a potent and selective antagonist that binds only to rat mGluR1 receptor and displays an IC50 of 128 nM for the rat receptor transfected in HEK 293 cells. It has a low affinity for human mGluR11.
    1. Malherbe, P. et al. (2003) J. Biol. Chem. 278, 8340.
    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 Up to 100 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs EM-TBPC inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs EM-TBPC inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Dose response of normalized inhibition of human mGluR1 receptors mediated, L-Glutamate evoked Ca2+ mobilization by EM-TBPC (#E-165). IC50 was determined at 370 nM. hmGluR1-expressing cells were loaded with Ca2+-sensitive dye, incubated with a range of concentrations of EM-TBPC, and stimulated by 15 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. Malherbe, P. et al. (2003) J. Biol. Chem. 278, 8340.
    2. Eom.HS. et al. (2016) PLoS One 11, e0147538.
    Scientific background

    EM-TBPC is a synthetic compound that acts as a potent, selective and noncompetitive antagonist of rat mGluR1 receptors with an IC50 value of 128 for rat mGluR1 expressed in HEK 293 cells. It displays very low affinity for human mGluR1 receptors. The binding pocket of EM-TBPC has been localized at the 7 transmembrane (7TM) domain of mGluR11.

    Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) that play an important role in synaptic plasticity and other neuro-physiological and pathological processes including a major role in central sensitization and neuropathic pain. Type 1 mGluRs are mainly expressed on post-synaptic neurons and are known to affect the fate of neuronal progenitor cells and neural stem cell and the formation of the hippocampus2.

    Target mGluR1
    Last update: 02/01/2022

    EM-TBPC (#E-165) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background

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