产品展示更多>>
- Danthron 117-10-2

- Danthron 117-10-2
Danthron 117-10-2
产品描述 描述 Danthron is a natural product, regulates glucose, and lipid metabolism by activating AMPK.纯度 >98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 1,8-二羟基蒽醌;丹蒽醌;Dantron;Chrysazin;1,8-Dihydroxyanthraquinone外观 黄色至橙色固体可溶性/溶解性 DMSO: 4 mg/mL (16.65 mM)生物活性 靶点 AMPKIn vitro(体外研究) Danthron (0.1, 1, and 10 μM) dose-dependently promotes the phosphorylation of AMPK and acetyl-CoA carboxylase (ACC) in both HepG2 and C2C12 cells. Meanwhile, Danthron treatment significantly reduces the lipid 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, Danthron treatment efficiently increases glucose consumption. Danthron effectively reduces intracellular lipid contents and enhances glucose consumption in vitro via activation of AMPK signaling pathway. 10 μM Danthron/24 h is safe for HepG2 cells. With 80% confluence, HepG2 cells are incubated with Danthron (0.1-10 μM) in FBS-Free media for 8 h. Subsequently, 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. Danthron inhibits 9-cis retinoic acid (9cRA)-induced retinoic X receptor α (RXRα) transactivation by IC50 at 0.11 μM. To further clarify the stoichimetric ratio of Danthron binding to RXRα-ligand-binding domain (LBD), isothermal titration calorimetry (ITC) experiment is performed. The KD value of Danthron binds to RXRα-LBD by ITC experiment is determined at 7.5 μM.In vivo(体内研究) Danthron functions as an insulin sensitizer in vivo. Danthron improves insulin sensitivity in diet-induced obese (DIO) mice. The insulin tolerance test result shows that Danthron (5 mg/kg) treated diet-induced obesity mice exhibit lower glucose levels after insulin challenge, compared with the control vehicle-treated group.参考文献 参考文献 1. Zhou R, et al. Acta Pharmacol Sin. 2013 Aug; 34(8):1061-9.
2. Chiou SM, et al. Neurochem Res. 2012 Aug; 37(8):1790-800.
3. Verebová V, et al. Biochem Biophys Res Commun. 2014 Jan 31;444(1):50-5.
研究领域 研究领域 EpigeneticsDrug DiscoverySmall Molecule DrugLead Compound DiscoveryDanthron 117-10-2温馨提示:本产品仅作科研实验使用,不支持临床等研究
