SR12813-GW-485801-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESR12813Cat. No.: HY-100793CAS No.: 126411-39-0Synonyms: GW 485801分式: CHOP分量: 504.53作靶點(diǎn): HMG-CoA Reductase (HMGCR); Autophagy作通路: Metabolic Enzyme/Protease; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C

2、1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (99.10 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.9820 mL 9.9102 mL 19.8204 mL5 mM 0.3964 mL 1.9820 mL 3.9641 mL10 mM 0.1982 mL 0.9910 mL 1.9820 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)?/p>

3、溶解案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.96 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.96 mM); Clear solutio

4、n1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 SR12813有效的3-羥-3-甲-戊酰輔酶A還原酶 (HMG-CoA reductase) 抑制劑，IC50 值為 0.85 M。IC50 & Target IC50: 0.85 M (HMG-CoA Reductase)體外研究 SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC50 of 1.2 M but has no effect on

5、fatty acid synthesis. Furthermore, SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC50 of 0.85 M 1. Both 25-HC and SR-12813 can kill mammalian cellsthrough blocking the synthesis of cholesterol, thereby they are ideal regents for lethal selection

6、. SR-12813kills HeLa cells at concentration range from 8 M to 16 M. SR-12813 kills wild type cells and mutant cellsinfected by Ad-Cre (SL-5+Cre), but the mutant SL-5 survives this condition. SR-12813 or 25-HC promotesthe degradation of the 95-KDa full-length HMG-CoA reductase in wild type HeLa and S

7、L-5 mutant cells 1.PROTOCOLKinase Assay 1 Briefly, compounds are added to the cells in Me2SO (final concentration, 0.1%). After the experiment cellsare lysed by the addition of 0.1 mL of 0.25% Brij 96, 0.1 M sucrose, 0.1 M KF, 50 mM KCl, 40 mM potassiumdihydrophosphate, 30 mM EDTA, 5 mM dithiothreit

8、ol, pH 7.4 at room temperature. In some experiments KFis omitted to measure “total” HMG-CoA reductase activity. HMG-CoA reductase activity in the cell lysate isfurther determined.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Berkhout T, e

9、t al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J Biol Chem. 1996 Jun 14;271(24):14376-82.2. Jiang W, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertionalmutagenesis. PLoS One. 2014 Nov 26;9(11):e112632.McePdfHeightCaution: Product has not been fully validated for m