A TRMP5 activator; induces inward and outward rectifying currents in TRPM3-expressing HEK293 cells voltage-clamped at ±80 mV at 1 µM; selective for TRMP3 over TRPM1

CIM0216 – 5 mg

Brand:
Cayman
CAS:
1031496-06-6
Storage:
-20
UN-No:
Non-Hazardous - /

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.{48910} 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.{48910} 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.{48911}  

 

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Description

A TRMP5 activator; induces inward and outward rectifying currents in TRPM3-expressing HEK293 cells voltage-clamped at ±80 mV at 1 µM; 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; 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; stimulates insulin and CGRP release in isolated mouse pancreatic islets and skin nerve terminals, respectively, from 5-100 µM; induces activation of AP-1, c-Jun, and c-fos in HEK293 cell reporter assays at 20 µM

Formal name: 3,4-dihydro-N-(5-methyl-3-isoxazolyl)-α-phenyl-1(2H)-quinolineacetamide

Synonyms: 

Molecular weight: 347.4

CAS: 1031496-06-6

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Epigenetics, Transcription, & Translation|Transcription Factors||Research Area|Neuroscience

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