CIM0216 是一种合成的 TRPM3 配体，是一种有效的选择性 TRPM3激动剂。CIM0216 对 TRPM3 的选择性高于 TRPM1、TRPM2 和 TRPM4-8。CIM0216 以TRPM3 依赖性的方式引起疼痛并唤起感觉神经末梢的神经肽释放。CIM0216 是研究 TRPM3 生理功能的有力工具，可用于神经源性炎症的相关研究。

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.

Solid

TRPM3

CIM0216 elicits a dose-dependent Ca 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 Ca concentration (1,145±26 nM) in single-cell FURA2-ratiometric Ca imaging in HEK-TRPM3 cells. These responses are not observed in nontransfected HEK cells or in the absence of extracellular Ca.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 35 mg/mL (100.75 mM; Need ultrasonic and warming)Ethanol : 17 mg/mL (48.93 mM; Need ultrasonic and warming)配制储备液