SB-204990 - ATP Citrate Lyase 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESB 204990Cat. No.: HY-16450CAS No.: 154566-12-8分式: CHClO分量: 389.27作靶點: ATP Citrate Lyase作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 10 mg/mL (25.69 mM; Need

2、 ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.5689 mL 12.8446 mL 25.6891 mL5 mM 0.5138 mL 2.5689 mL 5.1378 mL10 mM 0.2569 mL 1.2845 mL 2.5689 mL請根據(jù)產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。BIOLOGICAL ACTIVITY物活性 SB 204990是ATP檸檬酸裂解酶 (ACLY) 的有效特異性抑制劑。IC50 & Target ACLY 1.體外研究 SB20499

3、0 (SB) is a specific inhibitor of ACLY enzyme. SB204990 treatment leads to a decrease in cytosolicAc-CoA level and is thus expected to decrease acetylated and active -catenin levels 1.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體內研究 SB 204990, when administered orally to rats, is absorbed into

4、the systemic circulation. When administered inthe diet (0.05-0.25%, w/w) for 1 week, SB 204990 causes a dose-related decrease in plasma cholesterol (byup to 46%) and triglyceride levels (by up to 80%) in rats. SB 204990 (25 mg/kg per day) also decreasesplasma cholesterol levels (by up to 23%) and tr

5、iglyceride levels (by up to 38%) in the dog, preferentiallydecreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels 2.REFERENCES1. Shares BH, et al. Active mitochondria support osteogenic differentiation by stimulating -catenin acetylation. J Biol Chem. 2018 Oct12

6、;293(41):16019-16027.2. Pearce NJ, et al. The role of ATP citrate-lyase in the metabolic regulation of plasma lipids. Hypolipidaemic effects of SB-204990, alactone prodrug of the potent ATP citrate-lyase inhibitor SB-201076. Biochem J. 1998 Aug 15;334 ( Pt 1):113-9.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-