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ML 204
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML 204图片
CAS NO:5465-86-1
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
ML 204 是一种有效的选择性 TRPC4/TRPC5 通道抑制剂,对 TRPC6 的选择性至少是 19 倍,对所有其他 TRP 通道没有明显影响,对电压门控钠、钾或 Ca2+ 通道也没有明显影响。
Cas No.5465-86-1
化学名4-methyl-2-(piperidin-1-yl)quinoline
Canonical SMILESCC1=CC(N2CCCCC2)=NC3=CC=CC=C13
分子式C15H18N2
分子量226.32
溶解度DMF: 30 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 15 mg/ml,Ethanol: 15 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.IC50 value:Target: TRPC4/C5 inhibitorML204 inhibited TRPC4β-mediated intracellular Ca(2+) rise with an IC(50) value of 0.96 μm and exhibited 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation. In whole-cell patch clamp recordings, ML204 blocked TRPC4β currents activated through either μ-opioid receptor stimulation or intracellular dialysis of guanosine 5'-3-O-(thio)triphosphate (GTPγS), suggesting a direct interaction of ML204 with TRPC4 channels rather than any interference with the signal transduction pathways. Selectivity studies showed no appreciable block by 10-20 μm ML204 of TRPV1, TRPV3, TRPA1, and TRPM8, as well as KCNQ2 and native voltage-gated sodium, potassium, and calcium channels in mouse dorsal root ganglion neurons. 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 [1]. ML204 blocked TRPC4 channels in an electrophysiological assay with an IC value of 2.6 μM and was also active in fluorescent and electrophysiological assays in which TRPC4 channels were activated by different mechanisms, indicating direct block of TRPC4 channels. Selectivity for block of TRPC4 channels was examined in fluorescent and electrophysiological experiments against closely related TRPC channels and more distantly related TRPV, TRPA and TRPM channels, and against non-TRP ion channels. ML204 afforded good selectivity (19-fold) against TRPC6 channels and more modest selectivity against TRPC3 and TRPC5 (9-fold) channels [2].

References:
[1]. Miller M, et al. Identification of ML204, a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels. J Biol Chem. 2011 Sep 23;286(38):33436-46.
[2]. Miller MR, et al. Novel Chemical Inhibitor of TRPC4 Channels. Probe Reports from the NIH Molecular Libraries Program [Internet].