Every lot is tried & tested in a relevant biological assay.
- Ito, S. et al. (2009) Bioorg. Med. Chem. Lett. 19, 5310.
- 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™.
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.
MK-5435 (#M-265) is a highly pure, synthetic, and biologically active compound.