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MK-5435

DFMTI

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.
    Structure
    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.
    References-Activity
    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: 11/04/2021

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

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
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