FTIDC

Non Antibodies

mGluR1

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

358, 4

A Potent and Selective Antagonist of mGluR1 Receptors

Centrifuge the vial before adding solvent (10, 000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity

41116134

FTIDC is a potent and selective allosteric antagonist of the mGluR1 receptor, shown to inhibit L-glutamate-induced Ca2+ mobilization in human and mouse mGluR1a-expressing CHO cells (IC50 values of 5.8 nM and 3.1 nM, respectively), while having a 1000-fold weaker activity against human and rat mGluR5 (IC50 values of 6.2 µM and 9.9 µM, respectively)1.

Yes

FTIDC is a highly potent and selective allosteric antagonist of mGluR1 receptors and shows very weak potency against human and rat mGluR5 receptors. The inhibition of FTIDC for mGluR1 receptors is shown to be in noncompetitive manner and displays IC50 values of 5.8 and 3.1 nM for human and mouse mGluR1 expressed in CHO cells respectively1.Studies using chimeric and mutant mGluR1 show that transmembrane (TM) domains 4 to 7, play an important role in the antagonistic properties of FTIDC. The compound has oral activity on recombinant human, mouse, and rat mGluR1 without species differences in its antagonistic activity. The compound is considered to be a valuable tool for elucidating the functions of mGluR1 in rodents and in humans1, 2.Metabotropic glutamate receptors (mGluRs) are G-protein coupled receptors (GPCR) and 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 in somatodendritic domains and postsynaptically regulate neuronal excitability and synaptic transmission through several intracellular second messenger systems2, 3.