CIM0216

• CAT Number: I011229
• CAS Number: 1031496-06-6
• Molecular Formula: C21H21N3O2
• Molecular Weight: 347.41
• Purity: ≥95%
• Synonyms: 2-(3,4-dihydro-2H-quinolin-1-yl)-N-(5-methyl-1,2-oxazol-3-yl)-2-phenylacetamide
• InChI: InChI=1S/C21H21N3O2/c1-15-14-19(23-26-15)22-21(25)20(17-9-3-2-4-10-17)24-13-7-11-16-8-5-6-12-18(16)24/h2-6,8-10,12,14,20H,7,11,13H2,1H3,(H,22,23,25)
• InChIKey: KSEXDSJYVSEVGF-UHFFFAOYSA-N
• SMILES: CC1=CC(=NO1)NC(=O)C(C2=CC=CC=C2)N3CCCC4=CC=CC=C43

CIM0216, a synthetic TRPM3 ligand, acts as a potent and selective agonist of TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research[1].
CIM0216 elicits a dose-dependent Ca2+ response [pEC50=0.77±0.1 μM] in HEK-TRPM3 cells, which is not observed in nontransfected HEK293 cells. CIM0216 induces a robust increase in intracellular Ca2+ concentration (1,145±26 nM) in single-cell FURA2-ratiometric Ca2+ imaging in HEK-TRPM3 cells. These responses are not observed in nontransfected HEK cells or in the absence of extracellular Ca2+[1].
CIM0216 (10 μM) has no stimulating/blocking effect on TRPM1, TRPM4, TRPM6, or TRPM7 currents; however, a small blocking effect of CIM0216 is observed after activation of TRPM2 (16.6% block) and TRPM5 (33.5% block). CIM0216 also has no detectable effect on human TRPV1 and TRPM8 channel activation[1].

Reference

[1]. Katharina Held, et al. Activation of TRPM3 by a potent synthetic ligand reveals a role in peptide release. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):E1363-72.
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