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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEML-7 hydrochlorideCat. No.: HY-15417CAS No.: 110448-33-4分式: CHClINOS分量: 452.74作靶点: Myosin作通路: Cytoskeleton储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 43 mg/mL (94.98 mM)* means soluble,
2、 but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2088 mL 11.0439 mL 22.0877 mL5 mM 0.4418 mL 2.2088 mL 4.4175 mL10 mM 0.2209 mL 1.1044 mL 2.2088 mL请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 ML-7 hydrochloride种萘磺酰胺衍物,有效抑制 MLCK (IC50=300 nM)。IC50 & T
3、arget IC50: 300 nM (MLCK) 1体外研究ML-7 hydrochloride inhibits rabbit portal vein 1-adrenoceptor NSCC with IC50 of 0.8 M 1. The myosinlight chain kinase (MLCK) inhibitor ML-7 hydrochloride (3 M and 10 M) also attenuates the1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEDexmedetomidine (DMT)-induced co
4、ntraction (p 2.体内研究 In sham operated animals Evans Blue extravasation is not different between ML-7 hydrochloride and vehiclegroup (sham+vehicle: 0.260.02 OD/g; sham+ML-7: 0.260.02 OD/g). After CCI inhibition of MLCK with ML-7 results in a significant lower amount of intracerebral Evans Blue compare
5、d to vehicle treated animals(CCI+vehicle: 0.420.04 OD/g; CCI+ML-7: 0.350.05 OD/g, p=0.048) 3.PROTOCOLAnimal Mice 3Administration 3 Mice are treated with intraperitoneal injection of the selective MLCK inhibitor ML-7 (1 mg/kg) or vehiclesolution (0.9% NaCl,control group) 1 h prior to and 6 h after tr
6、auma. Hemispheric brain water content andneurological function are measured 24 h after controlled cortical impact (CCI) in animals randomized to: (i)vehicle+sham surgery, (ii) vehicle+CCI, (iii) ML-7+shamsurgery or (iv) ML-7+CCI (n=8 per group) and 15 minafter CCI in animals randomized to: (i) vehic
7、le+sham surgery, (ii) vehicle+CCI, (iii) ML-7+sham surgery or (iv)ML-7+CCI (n=6 per group). Mice are treated with intraperitoneal injection of the selective MLCK inhibitor ML-7 (1 mg/kg) or vehicle solution (0.9% NaCl, control group) 1 h prior to and 6 h after trauma. Evans Blueextravasation is dete
8、rmined 24 h after surgery in animals randomized to: (i) vehicle + CCI or (ii) ML-7+CCI(n=5 per group) and in animals randomized to (iii) vehicle + sham surgery or (iv) ML-7+sham surgery (n=6per group). ICP is measured 24 h CCI and sham surgery.MCE has not independently confirmed the accuracy of thes
9、e methods. They are for reference only.户使本产品发表的科研献 Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Shi J, et al. Myosin light chain kinase-independent inhibition by ML-9 of murine TRPC6 channels expressed in HEK293cells. Br JPharmacol. 2007 S
10、ep;152(1):122-31.2. Yu J, et al. Dexmedetomidine-Induced Contraction in the Isolated Endothelium-Denuded Rat Aorta Involves PKC-mediated JNKPhosphorylation. Int J Med Sci. 2015 Sep 4;12(9):727-363. Luh C, et al. Inhibition of myosin light chain kinase reduces brain edema formation after traumatic brain injury. J Neurochem. 2010Feb;112(4):1015-25.McePdfHeightCaution: Product has not been fully v
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