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A Potent and Selective Antagonist of mGluR1 Receptors

Cat #: C-365
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 349.4
    Purity: >96%
    Effective concentration 10 nM – 10 µM.
    Chemical name 2-cyclopropyl-5-[1-(2-fluoropyridin-3-yl)-5-methyltriazol-4-yl]-3H-isoindol-1-one.
    Molecular formula C19H16FN5O.
    CAS No.: 864864-17-5
    PubChem CID 11175501
    Activity CFMTI is a selective and potent allosteric antagonist of mGluR1 receptors. It inhibits L-glutamate-induced intracellular Ca2+ mobilization in CHO cells expressing human and rat mGluR1a with IC50 values of 2.6 and 2.3 nM, respectively. It is highly selective for mGluR1 over mGluR5 (2000-fold), and does not affect mGluR subtypes and other receptors at 10 µM1.
    1. Satow, A. et al. (2008) J. Pharmacol. Exp. Ther.  326, 577.
    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 10 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs CFMTI inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs CFMTI inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Dose-response of normalized inhibition of human mGluR1 mediated, L-glutamate evoked Ca2+ mobilization by CFMTI (#C-365), showing complete inhibition at 10 µM. hmGluR1-expressing cells were loaded with Ca2+-sensitive dye, incubated with different concentrations of CFMTI, 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. Suzuki, G. et al. (2007) J. Pharmacol. Exp. Ther. 321, 1144.
    2. Satow, A. et al. (2008) J. Pharmacol. Exp. Ther.  326, 577.
    3. Eom, H.S. et al. (2016) PLoS One 11, e0147538.
    Scientific background

    CFMTI is a negative allosteric modulator of mGluR1 receptors with IC50 values of 2.6 and 2.3 nM for human and rat mGluR1 expressed in CHO cells, respectively. CFMTI demonstrates high potency and selectivity for the receptor both in vitro and in vivo after oral administration and shows very low potency for other mGluR subtypes1,2.

    Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCRs) 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 cells and the formation of the hippocampus3.

    Target mGluR1
    Last update: 06/11/2022

    CFMTI (#C-365) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background

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