EX229 - AMPK Activator - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEX229Cat. No.: HY-112769CAS No.: 1219739-36-2分式: CHClNO分量: 431.87作靶点: AMPK作通路: Epigenetics; PI3K/Akt/mTOR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 : 13 mg/mL (30.10 mM; Need ultrasonic

2、and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3155 mL 11.5776 mL 23.1551 mL5 mM 0.4631 mL 2.3155 mL 4.6310 mL10 mM 0.2316 mL 1.1578 mL 2.3155 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

3、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: 1.3 mg/mL (3.01 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.3 mg/mL (3.01 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 1.3 mg/mL (3.01 mM)

4、; Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 EX229个苯并咪唑的衍物， AMP 活化蛋激酶 (AMPK) 的有效变构激动剂，其对 111、211 和 121 的 Kd 值分别为 0.06 M、0.06 M 和 0.51 M。IC50 & Target AMPK 111 AMPK 211 AMPK 1210.06 M (Kd) 0.06 M (Kd) 0.51 M (Kd)体外研究 EX229 is a potent and allosteric activato

5、r of AMP-activated protein kinase (AMPK), with Kds of 0.06 M, 0.06M and 0.51 M for 111, 211 and 121, respectively. 1. Treatment of hepatocytes with EX229(991) alone results in a slight increase in the phosphorylation of AMPK and RAPTOR only at 0.3 M,whereas a robust increase in ACC phosphorylation i

6、s readily observed and saturated at a concentration of0.03 M EX229. AICAR or C13 alone robustly increases T172 phosphorylation of AMPK, and when 991 iscoincubated, there is a modest additional dose-dependent increase in AMPK phosphorylation. RAPTORphosphorylation is modestly increased by AICAR or C1

7、3 alone, and it is dose dependently increased whencoincubations are carried out with EX229. EX229 also dose dependently (0.01 and 0.1 M) inhibitslipogenesis (34% and 63%, respectively), which is further reduced when it is coincubated with a low dose ofAICAR (0.03 mM) or C13 (1 M). Treatment with EX2

8、29 promotes dose-dependent increases in ACC andRAPTOR phosphorylation. Similar to the observations in hepatocytes 2.REFERENCES1. Xiao B, et al. Structural basis of AMPK regulation by small molecule activators. Nat Commun. 2013;4:3017.2. Bultot L, et al. Benzimidazole derivative small-molecule 991 enhances AMPK activity and glucose uptake induced by AICAR orcontraction in skeletal muscle. Am J Physiol Endocrinol Metab. 2016 Oct 1;311(4):E706-E719.McePdfHeightCaution: Product has not been fully validated for medical appl