化合物CIM0216 T9263

Product Introduction
Bioactivity


英文名: cim0216

描述: CIM0216 是选择性的TRPM3激动剂，对 TRPM3 的选择性高于 TRPM1、TRPM2 和 TRPM4-8。它以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，可用于神经源性炎症的相关研究。

体外活性: CIM0216 Selectively Activates TRPM3 in Stably Transfected HEK293 Cells.A diverse small-molecule library was screened for compounds that modulate TRPM3-mediated Ca2+ responses in HEK293 cells stably expressing murine TRPM3 (HEK-TRPM3 cells), as described previously[1].In HEK-TRPM3 cells, CIM0216 elicited a dose-dependent Ca2+ response [negative logarithm of the EC50 value (pEC50) = 0.77 ± 0.1 μM], which was not observed in nontransfected HEK293 cells . The endogenous TRPM3 activator pregnenolone sulfate (PS) also elicited a dose-dependent Ca2+ response, typified by a smaller Ca2+ influx and a fivefold lower potency (pEC50 = 3.0 ± 0.1 μM; n = 2) compared with CIM0216 . In the presence of 40 μM PS, the dose dependency of CIM0216 shifted to a lower concentration in HEK-TRPM3 cells (pEC50 = 42 ± 0.6 nM CIM0216 in the presence of PS). Single-cell FURA2-ratiometric Ca2+ imaging revealed a robust increase in intracellular Ca2+ concentration (1,145 ± 26 nM; n = 603 from at least three independent measurements) on stimulation with 1 μM CIM0216 in all HEK-TRPM3 cells. These responses were not observed in nontransfected HEK cells (n = 166) or in the absence of extracellular Ca2+.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 30 mg/mL (86.35 mM)
Ethanol : 17 mg/mL (48.93 mM)


关键字: cim-0216 | inflammation | inhibit | TRP Channel | cim0216 | Transient receptor potential channels | sensory nerve | neurogenic | TRPM3 | Inhibitor | CIM 0216

相关产品: GFB-8438 | Caffeic Acid | Optovin | RN-1747 | Hydroxy-α-sanshool | Mavatrep | GSK1016790A | D-GsMTx4 TFA | ABT-239 | TRPV3 antagonist 74a

相关库: Ion Channel Inhibitor Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | NO PAINS Compound Library | Bioactive Compound Library

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