Name: MK-5435
Brand: Alomone Labs
SKU: M-265

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

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.
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 FLIPR^TETRA™.

References - Scientific background

Hostetler, E.D . et al. (2011) Synapse 65, 125.
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

Lyophilized Powder

Last update: 02/01/2022

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

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MK-5435

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