CAS:5465-86-1ML204

ML204 is a selective antagonist of TRPC4 ion channel with IC50 of 0.96 μM and 2.6 μM in fluorescent and electrophysiological assays respectively.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

5465-86-1

储存条件

分子式

C15H18N2

运输

蓝冰

分子量

226.32

别名

溶解度

DMSO	129.0 mg/mL (570.0 mM)
Water	insoluble

动物实验配方

生物活性

描述Transient receptor potential canonical (TRPC) channels are Ca²⁺-permeable nonselective cation channels implicated in diverse physiological functions, including smooth muscle contractility and synaptic transmission. ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC₅₀ values of about 1 μM in fluorescent intracellular Ca²⁺ assays and about 3 μM in whole-cell voltage clamp experiments. ML204 blocked TRPC4β activity induced through either G_i/o stimulation by μ-opioid, 5HT_1A serotonin, and M₂ muscarinic receptors or G_q/11 stimulation by the endogenous M₃-like muscarinic receptors. It also blocked TRPC4β channels activated by intracellularly applied GTPγS (guanosine 5'-3-O-(thio) triphosphate) or Ca²⁺, which bypass receptor stimulation. In isolated guinea pig ileal myocytes, ML204 blocked muscarinic cation currents activated by bath application of carbachol or intracellular infusion of GTPγS, demonstrating its effectiveness on native TRPC4 currents.