|1-(5-碘萘-1-磺酰基)-1H-六氢-1,4-二氮杂卓盐酸盐|CsnPharm

CAS No.: 110448-33-4

ML-7 HCl Catalog No. CSN12294

Synonyms: ML-7 (hydrochloride);ML-7 HCl;ML-7

ML-7 HCl is a multiple-target inhibitor of MLCK with Ki value of 300 nM, PKA with 21μM, and PKC of 42 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Myosin light chain kinase (MLCK) is a serine/threonine-specific protein kinase that plays a key role in regulating the actin-myosin interaction of smooth muscles. ML-7 is a naphthalene sulphonamide derivative that inhibits MLCK with an IC50 value of 300nM. It also shows inhibitory activities against rabbit portal vein α1-adrenoceptor non-selective cation channel with an IC50 value of 0.8μM^[3]. In a mouse model of controlled cortical impact, specific inhibition of MLCK by ML-7 (1mg/kg; i.p. injection) significantly reduced post-traumatic brain edema formation and intracranial hypertension, decreased permeability of the brain-blood barrier, and suppressed phosphorylation of myosin light chains compared with vehicle-treated animals^[4].
参考文献

[1] Cheng X, Wang X, et al. Myosin light chain kinase inhibitor ML7 improves vascular endothelial dysfunction via tight junction regulation in a rabbit model of atherosclerosis. Mol Med Rep. 2015 Sep;12(3):4109-16.
[2] Saitoh M, Ishikawa T, et al. Selective inhibition of catalytic activity of smooth muscle myosin light chain kinase. J Biol Chem. 1987 Jun 5;262(16):7796-801.
[3] Shi J, Takahashi S, Jin XH, et al. Myosin light chain kinase-independent inhibition by ML-9 of murine TRPC6 channels expressed in HEK293 cells. Br J Pharmacol. 2007;152(1):122-131.
[4] Luh C, Kuhlmann CR, Ackermann B, et al. Inhibition of myosin light chain kinase reduces brain edema formation after traumatic brain injury. J Neurochem. 2010;112(4):1015-1025.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2088 mL
- 11.0439 mL
- 22.0878 mL
- 5 mM
- 0.4418 mL
- 2.2088 mL
- 4.4176 mL
- 10 mM
- 0.2209 mL
- 1.1044 mL
- 2.2088 mL

技术信息

CAS号

110448-33-4

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H18ClIN2O2S

运输

蓝冰

分子量

452.74

别名

ML-7 (hydrochloride);ML-7 HCl;ML-7

溶解度

DMSO	90.0 mg/mL (198.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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