CAS NO: | 1031496-06-6 |
生物活性 | CIM0216, a syntheticTRPM3ligand, 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 terminalsin vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research[1]. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (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]. | ||||||||||||||||
分子量 | 347.41 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C21H21N3O2 | ||||||||||||||||
CAS 号 | 1031496-06-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | 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
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