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. 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. 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.Formal Name: 3,4-dihydro-N-(5-methyl-3-isoxazolyl)-alpha-phenyl-1(2H)-quinolineacetamide. CAS Number: 1031496-06-6. Molecular Formula: C21H21N3O2. Formula Weight: 347.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: slightly soluble, Methanol: slightly soluble. SMILES: CC1=CC(NC(C(N2C3=CC=CC=C3CCC2)C4=CC=CC=C4)=O)=NO1. InChi Code: 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). InChi Key: KSEXDSJYVSEVGF-UHFFFAOYSA-N.