Catalog No.: PC-24729Not For Human Use, Lab Use Only.
CIM0216 is a potent, selective synthetic TRPM3 activator / agonist, evokes robust increases in intracellular Ca2+ concentration in HEK-TRPM3 cells with EC50 of 0.77 uM.
CIM0216 is a potent, selective synthetic TRPM3 activator / agonist, evokes robust increases in intracellular Ca2+ concentration in HEK-TRPM3 cells with EC50 of 0.77 uM. CIM0216 exceeds the potency and apparent affinity of canonical TRPM3 agonist, pregnenolone sulfate (PS) (EC50=3.0 uM). CIM0216 (10 uM) has no stimulating/blocking effect on TRPM1, TRPM4, TRPM6, or TRPM7 currents, and weak activity against TRPM2 (16.6% block) and TRPM5 (33.5% block). CIM0216 modualtes PS-induced TRPM3 currents with EC50 of 42 nM in HEK-TRPM3 cells. CIM0216 evoked robust calcium influx in TRPM3-expressing somatosensory neurons, and intradermal injection of the compound induced a TRPM3-dependent nocifensive behavior. CIM0216 elicited the release of the peptides calcitonin gene-related peptide (CGRP) from sensory nerve terminals and insulin from isolated pancreatic islets in a TRPM3-dependent manner.
