Danthron-Dantron-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDanthronCat. No.: HY-B0923CAS No.: 117-10-2Synonyms: Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone分式: CHO分量: 240.21作靶點(diǎn): AMPK; Autophagy作通路: Epigenetics; PI3K/Akt/mTOR; Autophagy儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C

2、6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 42 mg/mL (174.85 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 4.1630 mL 20.8151 mL 41.6302 mL5 mM 0.8326 mL 4.1630 mL 8.3260 mL10 mM 0.4163 mL 2.0815 mL 4.1630 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGIC

3、AL ACTIVITY物活性 Danthron種從中藥 rhubarb 中提取的天然產(chǎn)物。Danthron 通過(guò)激活 AMPK 來(lái)調(diào)節(jié)葡萄糖和脂質(zhì)代謝。IC50 & Target AMPK體外研究Danthron (0.1, 1, and 10 M) dose-dependently promotes the phosphorylation of AMPK and acetyl-CoA1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEcarboxylase (ACC) in both HepG2 and C2C12 cells. Meanwhil

4、e, Danthron treatment significantly reduces thelipid synthesis related sterol regulatory element-binding protein 1c (SREBP1c) and fatty acid synthetase(FAS) gene expressions, and the total cholesterol (TC) and triglyceride (TG) levels. In addition, Danthrontreatment efficiently increases glucose con

5、sumption. Danthron effectively reduces intracellular lipid contentsand enhances glucose consumption in vitro via activation of AMPK signaling pathway. 10 M Danthron/24 his safe for HepG2 cells. With 80% confluence, HepG2 cells are incubated with Danthron (0.1-10 M) in FBS-Free media for 8 h. Subsequ

6、ently, cells are harvested for Western blot assay. Danthron increases the p-AMPK protein in a dose-dependent manner, and no changes in t-AMPK protein are observed 1. Danthroninhibits 9-cis retinoic acid (9cRA)-induced retinoic X receptor (RXR) transactivation by IC50 at 0.11 M.To further clarify the

7、 stoichimetric ratio of Danthron binding to RXR-ligand-binding domain (LBD), isothermaltitration calorimetry (ITC) experiment is performed. The KD value of Danthron binds to RXR-LBD by ITCexperiment is determined at 7.5 M 2.體內(nèi)研究 Danthron functions as an insulin sensitizer in vivo. Danthron improves

8、insulin sensitivity in diet-inducedobese (DIO) mice. The insulin tolerance test result shows that Danthron (5 mg/kg) treated diet-inducedobesity mice exhibit lower glucose levels after insulin challenge, compared with the control vehicle-treatedgroup 2.PROTOCOLCell Assay 1 HepG2 cells are transfecte

9、d with pGL3-ABCA1 promoter-luc or pGL3-ABCG1 promoter-luc and pRL-SV40plasmids. At 6 h post-transfection, the cells are incubated with Danthron (0-20 M), TO90 (2 M) or DMSOfor 24 h. Luciferase activity is measured using the Dual Luciferase Reporter Assay kit 1.MCE has not independently confirmed the

10、 accuracy of these methods. They are for reference only.Animal Mice 2Administration 2 C57/BL6 male mice are fed with a high fat diet for 3 months and treated with Danthron (5 mg/kg) or vehicleorally for 8 weeks. The animals are then fasted for 6 h and then given intraperitoneal injection of insulin

11、at 1.5units/kg. Blood samples are analyzed at 15, 30, 45, 60, 90, and 120 min using Accu-Chek active blood sugartest meter.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zhou R, et al. Danthron activates AMP-activated protein kinase and regulates lipid and glucose metabolism in vitro. Acta Pharmacol Sin.2013 Aug;34(8):1061-9.2. Zhang H, et al. Danthron functions as a retinoic X receptor antagonist by stabilizing tetramers of the receptor. J Biol Chem. 2011 Jan21;286(3):1868-75.McePdfHeightCaution: Prod