Danthron
Cat.No:ID0070 Solarbio
CAS:117-10-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥97%
Appearance:Yellow to orange Solid
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PI3K/Akt/mTOR >
DanthronCAS:117-10-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥97%
Appearance:Yellow to orange Solid
Qty:
Size:
CAS | 117-10-2 |
Name | Danthron |
Molecular Formula | C14H8O4 |
Molecular Weight | 240.21 |
Solubility | Soluble in DMSO ≥10mg/mL |
Purity | HPLC≥97% |
Appearance | Yellow to orange Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 204-173-5 |
MDL | MFCD00001211 |
SMILES | O=C1C2=C(C=CC=C2O)C(C3=CC=CC(O)=C13)=O |
InChIKey | QBPFLULOKWLNNW-UHFFFAOYSA-N |
InChI | InChI=1S/C14H8O4/c15-9-5-1-3-7-11(9)14(18)12-8(13(7)17)4-2-6-10(12)16/h1-6,15-16H |
PubChem CID | 2950 |
Target Point | AMPK |
Passage | PI3K/Akt/mTOR;Epigenetics |
Background | Danthron regulates glucose and lipid metabolism by activating AMPK. |
Biological Activity | Danthron 通过激活 AMPK 来调节葡萄糖和脂质代谢[1-2]。 |
In Vitro | Danthron(0.1,1和10μM)剂量依赖性地促进HepG2和C2C12细胞中AMPK和乙酰辅酶A羧化酶(ACC)的磷酸化。同时,Danthron治疗显著降低了脂质合成相关的固醇调节元件结合蛋白1c(SREBP1c)和脂肪酸合成酶(FAS)基因的表达,以及总胆固醇(TC)和甘油三酯(TG)水平。此外,Danthron治疗有效地增加了葡萄糖消耗。 Danthron通过激活AMPK信号通路有效降低细胞内脂质含量并增强体外葡萄糖消耗。 10μMDanthron/ 24小时对HepG2细胞是安全的。在80%汇合的情况下,将HepG2细胞与Danthron(0.1-10μM)在无FBS培养基中孵育8小时。随后,收获细胞用于Western印迹分析。 Danthron以剂量依赖性方式增加p-AMPK蛋白,并且未观察到t-AMPK蛋白的变化[1]。 Danthron通过IC50在0.11μM抑制9-顺式视黄酸(9cRA)诱导的视黄酸X受体α(RXRα)反式激活。为了进一步阐明Danthron与RXRα-配体结合结构域(LBD)结合的化学计量比,进行等温滴定量热法(ITC)实验。 Danthron通过ITC实验与RXRα-LBD结合的KD值确定为7.5μM[2]。 |
In Vivo | Danthron在体内起胰岛素增敏剂的作用。 Danthron改善饮食诱导的肥胖(DIO)小鼠的胰岛素敏感性。胰岛素耐量试验结果显示,与对照载体治疗组相比,Danthron(5mg/kg)治疗的饮食诱导的肥胖小鼠在胰岛素攻击后表现出较低的葡萄糖水平[2]。 |
Cell Experiment | 用pGL3-ABCA1启动子-luc或pGL3-ABCG1启动子-luc和pRL-SV40质粒转染HepG2细胞。在转染后6小时,将细胞与Danthron(0-20μM),TO90(2μM)或DMSO孵育24小时。使用Dual Luciferase Reporter Assay试剂盒[1]测量荧光素酶活性。 |
Animal Experiment | 给小鼠[2] C57/BL6雄性小鼠喂食高脂肪饮食3个月,并用Danthron(5mg/kg)或载体口服治疗8周。然后将动物禁食6小时,然后以1.5单位/ kg腹膜内注射胰岛素。使用Accu-Chek活性血糖测试仪在15,30,45,60,90和120分钟分析血液样品。 |
Data Literature Source | [1]. 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 Jan 21;286(3):1868-75 |
Unit | Bottle |
Specification | 10mM*1mL in DMSO 50mg 100mg |
Danthron 通过激活 AMPK 来调节葡萄糖和脂质代谢。
Remark:These protocols are for reference only. Solarbio does not independently validate these methods.
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