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A Potent and Selective Antagonist of mGluR1 Receptors

Cat #: M-265
Alternative Name DFMTI
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 368.39
    Purity: >98%
    Effective concentration 10 nM – 10 µM.
    Chemical name 5-[1-(2,4-difluorophenyl)-5-methyltriazol-4-yl]-2-propan-2-yl-3H-isoindol-1-one.
    Molecular formula C20H18F2N4O.
    PubChem CID 15985251
    Activity MK-5435 is a potent and selective allosteric mGluR1 antagonist, inhibiting human and rat mGluR1 with IC50 of 4.3 and 3.6 nM, respectively. It is selective over mGluR5 (IC50 = 1.5 µM), mGluR2 and mGluR8 (IC50 = 10 µM), and has no affinity for the quisqualic binding site (IC50 >10 µM). in vivo, following an oral dose of 1 mg/kg,  plasma and brain concentrations in mice were 0.17 µM and 0.45 nmol/g respectively, at 30 min post-dose1.
    1. Ito, S. et al. (2009) Bioorg. Med. Chem. Lett. 19, 5310.
    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 25 mM in DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions -20°C.
    Our bioassay
    • Alomone Labs MK-5435 inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Alomone Labs MK-5435 inhibits mGluR1 mediated Ca2+ mobilization in U2OS cells.
      Dose-response of normalized inhibition of human mGluR1 mediated, L-Glutamate evoked Ca2+ mobilization by MK-5435 (#M-265), showing complete inhibition at 10 µM. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with a range of concentrations of MK-5435, 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. Hostetler, E.D. et al. (2011) Synapse 65, 125.
    2. Eom, H.S. et al. (2016) PLoS One 11, e0147538.
    Scientific background

    MK-5435 is an allosteric negative modulator of mGluR1 receptors. This synthetic compound demonstrates high potency and selective antagonistic activities towards the receptor with IC50 values of 4.3 ­+ 1.3 nM1.

    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 found 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 receptor
    Last update: 02/01/2022

    MK-5435 (#M-265) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background

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