ML-7 HCl

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Chemical Structure| 110448-33-4 同义名 : ML-7 (hydrochloride); ML-7 hydrochloride; ML-7
CAS号 : 110448-33-4
货号 : A121204
分子式 : C15H18ClIN2O2S
纯度 : 99%+
分子量 : 452.74
MDL号 : MFCD00065524
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 :

DMSO: 45 mg/mL(99.4 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.21 mM)，配合低频超声助溶
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.04mL

2.21mL

1.10mL

22.09mL

4.42mL

2.21mL
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.