ML204

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Chemical Structure| 5465-86-1 同义名 : CID-230710; NSC 25850; 2-piperidino-Lepidine
CAS号 : 5465-86-1
货号 : A835423
分子式 : C15H18N2
纯度 : 99%+
分子量 : 226.32
MDL号 : MFCD00817920
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
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[3]. 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[3]. ML204 blocked TRPC4β activity induced through either Gi/o stimulation by μ-opioid, 5HT1A serotonin, and M2 muscarinic receptors or Gq/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[3]. 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[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.42mL

0.88mL

0.44mL

22.09mL

4.42mL

2.21mL

44.19mL

8.84mL

4.42mL

参考文献

[1]Miller M, Shi J, 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, Shi J, et al. Novel Chemical Inhibitor of TRPC4 Channels. 2010 Dec 15 [updated 2011 May 26] .

[3]https://pubmed.ncbi.nlm.nih.gov/21795696/