1031496-06-6

1031496-06-6 structure

Name: CIM 0216
Chemical Name: CIM0216
CAS Number: 1031496-06-6
Molecular Formula: C₂₁H₂₁N₃O₂
Molecular Weight: 347.410
Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
Create Date: 2021-05-25 17:45:03
Modify Date: 2024-01-03 17:29:30
CIM0216, a potent and selective agonist of TRPM3, has the ability to open two distinct cation-permeable pores in TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts as a powerful tool for use in investigating the physiological roles of TRPM3, and can be used for neurogenic inflammation research[1].

Name	CIM0216
Synonyms	2-(3,4-Dihydro-1(2H)-quinolinyl)-N-(5-methyl-1,2-oxazol-3-yl)-2-phenylacetamide MFCD10627035 CIM0216 1(2H)-Quinolineacetamide, 3,4-dihydro-N-(5-methyl-3-isoxazolyl)-α-phenyl-

Description	CIM0216, a potent and selective agonist of TRPM3, has the ability to open two distinct cation-permeable pores in TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts as a powerful tool for use in investigating the physiological roles of TRPM3, and can be used for neurogenic inflammation research[1].
Related Catalog	Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel Research Areas >> Neurological Disease
Target	TRPM3
In Vitro	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].
References	[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.