GSK429286A - ROCK 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGSK429286ACat. No.: HY-11000CAS No.: 864082-47-3分式: CHFNO分量: 432.37作靶点: ROCK作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt; TGF-beta/Smad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 : 51 mg/mL

2、(117.95 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3128 mL 11.5642 mL 23.1283 mL5 mM 0.4626 mL 2.3128 mL 4.6257 mL10 mM 0.2313 mL 1.1564 mL 2.3128 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。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验

3、结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.81 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.81 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90%

4、 corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.08 mg/mL (4.81 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 GSK429286A是选择性的 ROCK1 抑制剂，IC50 值为14 nM。IC50 & Target ROCK1 RSK p70S6K14 nM (IC50) 780 nM (IC50) 1940 nM (IC50)体外研究 GSK429286A at 1 M reduces ROCK2 activity over 20-fold, u

5、nder conditions in which the only other kinasetested that is significantly inhibited is MSK1 whose activity is reduced 5-fold. GSK429286A is a moreselective ROCK2 inhibitor than the widely utilized ROCK inhibitor Y-27632 as assessed on kinase-specificitypanel, and does not significantly inhibit LRRK

6、2 even at doses as high as 30 M (500-fold higher than IC50 ofinhibition of ROCK2). GSK429286A slightly inhibits RSK and p70S6K with IC50 of 0.78 M and 1.94 M,respectively. GSK429286A significantly inhibits rat aortic ring dilation with IC50 of 190 nM 2.体内研究 GSK429286A has 61% oral bioavailability in

7、 male Sprague-Dawley rats. Oral administration of GSK429286Aat single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensiverats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2hours treatment at dose of 30 mg/kg 1

8、.PROTOCOLAnimal Rats: Spontaneously hypertensive rats (SHRs) are treated with GSK429286A to establish its effect on meanAdministration 1 arterial pressure. Compound is administered by single dose oral gavage (3, 10, 30 mg/kg) 1.MCE has not independently confirmed the accuracy of these methods. They

9、are for reference only.户使本产品发表的科研献 Patent. US20180263995A1. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan11;50(1):6-9.2. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinsons disease. Biochem J. 2009 Oct23;424(1):47-60.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not been fully validated