Bempedoic-acid-ETC-1002-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBempedoic acidCat. No.: HY-12357CAS No.: 738606-46-7Synonyms: ETC-1002; ESP-55016分式: CHO分量: 344.49作靶点: ATP Citrate Lyase; AMPK作通路: Metabolic Enzyme/Protease; Epigenetics; PI3K/Akt/mTOR储存式: Powder -20C 3 years4C 2 yearsIn solvent

2、 -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (290.28 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9028 mL 14.5142 mL 29.0284 mL5 mM 0.5806 mL 2.9028 mL 5.8057 mL10 mM 0.2903 mL 1.4514 mL 2.9028 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

3、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: 2.5 mg/mL (7.26 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.26 mM); Clear soluti

4、on3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (7.26 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Bempedoic acid (ETC-1002)种 ATP-柠檬酸裂解酶 (ATP-citrate lyase (ACL) 抑制剂 1。Bempedoic acid(ETC-1002) 激活 AMPK 2。IC50 & Target AMPK体外研究 Bempedoic acid (E

5、TC-1002) activates AMP-activated protein kinase in a Ca2+/calmodulin-dependent kinase-independent and liver kinase 1-dependent manner, without detectable changes in adenylate energycharge. Bempedoic acid is shown to rapidly form a CoA thioester in liver, which directly inhibits ATP-citratelyase 1. I

6、n cells treated with Bempedoic acid (ETC-1002), increased levels of AMP-activated protein kinase(AMPK) phosphorylation coincide with reduced activity of MAP kinases and decreased production ofproinflammatory cytokines and chemokines 2.体内研究 A marked and sustained increase in AMPK and ACC phosphorylat

7、ion is found in rat livers following twoweeks of treatment with Bempedoic acid (ETC-1002). Bempedoic acid is 100-fold more prevalent than theCoA thioester in rat liver and is associated with AMPK activation 1. Bempedoic acid (ETC-1002) suppressesthioglycollate-induced homing of leukocytes into mouse

8、 peritoneal cavity. In a mouse model of diet-inducedobesity, Bempedoic acid restores adipose AMPK activity, reduces JNK phosphorylation, and diminishesexpression of macrophage-specific marker 4F/80 2.PROTOCOLCell Assay 1 Glucose production is measured in primary rat hepatocyte cultures. Cells are cu

9、ltured in glucose- and phenolred-free DMEM, containing 10 mM lactate, 1 mM pyruvate, and nonessential amino acids. Cells areincubated with various concentrations of Bempedoic acid (0.1 to 100 M) 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal R

10、ats: Prior to single-dose Bempedoic acid administration, Male Wistar Han rats are fasted for 48 h and refedAdministration 1 a high-carbohydrate diet for an additional 48 h. For two-week assessment, rats are maintained on standardchow diet and dosed by oral gavage with Bempedoic acid at 30 mg/kg/day

11、for two weeks in the morning.Following nutritional staging and/or dosing, food is withdrawn 2 h prior to last the oral dose of ehicle controlor Bempedoic acid 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Pinkosky SL, et al. AMP-activat

12、ed protein kinase and ATP-citrate lyase are two distinct molecular targets for ETC-1002, a novel smallmolecule regulator of lipid and carbohydrate metabolism. J Lipid Res. 2013 Jan;54(1):134-51.2. Filippov S, et al. ETC-1002 regulates immune response, leukocyte homing, and adipose tissue inflammation via LKB1-dependent2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEactivation of macrophage AMPK. J Lipid Res. 2013 Aug;54(8):2095-108.McePdfHeightCau