MK-5435

S. Molecules

Israel

Storage as Solution: -20°C. - Storage after Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Lyophilized powder.

DFMTI - A Potent and Selective Antagonist of mGluR1 Receptors

7, 4

15985251

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.

Yes

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.