CIM0216

CIM0216 is a transient receptor potential melastatin 3 (TRPM3) activator. It induces inward and outward rectifying currents in TRPM3-expressing HEK293 cells voltage-clamped at ±80 mV when used at a concentration of 1 µM.¹ CIM0216 is selective for TRMP3 over TRPM1, TRPM4, TRPM6, and TRMP7 in HEK293 cells expressing the human channels, but does activate TRPA1 by 15% in CHO cells expressing mouse TRPA1 at 10 µM. CIM0216 also inhibits ADP-ribose-induced TRPM2, calcium-induced TRMP5, and methanol-induced TRPM8 activation by 17, 34, and 61%, respectively, in HEK293 cells expressing the human channels at 10 µM. It stimulates insulin and calcitonin gene-related peptide (CGRP) release in isolated mouse pancreatic islets and skin nerve terminals, respectively, when used at concentrations ranging from 5 to 100 µM.¹ CIM0216 (20 µM) induces activation of the TRPM3 signal transduction transcription factor AP-1 and its subunits, c-Jun and c-fos, in HEK293 cell reporter assays.²

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1. Held, K., Kichko, T., De Clercq, K., et al. Activation of TRPM3 by a potent synthetic ligand reveals a role in peptide release. Proc. Natl. Acad. Sci. USA 112(11), E1363-E1372 (2015).

2. Rubil, S., and Thiel, G. Activation of gene transcription via CIM0216, a synthetic ligand of transient receptor potential melastatin-3 (TRPM3) channels. Channels (Austin) 11(1), 79-83 (2017).