产品
编 号:F014108
分子式:C21H21N3O3
分子量:363.41
产品类型
结构图
CAS No: 1031195-19-3
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产品详情
生物活性:
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE-/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases.
体内研究:
E1231(40 mg/kg;口服;每天一次,连续 7 天)调节用 HFD 饮食喂养的金仓鼠的胆固醇和脂质代谢。E1231(25、50 和 100 毫克/千克,在 0.5% CMC-Na 中;口服;每天一次,持续 12 周)减少 ApoE-/- 中的动脉粥样硬化发展,没有肝毒性或肾毒性 /i> 用致动脉粥样化饮食喂养的小鼠。Animal Model:HFD-diet Golden hamsters (80-90 g)
Dosage:40 mg/kg
Administration:PO; once daily for 7 days
Result:Increased SIRT1 protein expression but not SIRT3, SIRT6, or SIRT7. And reduced liver and serum cholesterol in hamsters.
Animal Model:Atherogenic diet ApoE-/- mice
Dosage:25, 50, and 100 mg/kg
Administration:PO; once daily for 12 weeks
Result:Modulated plaque composition, immunofluorescence staining. And reduced CD68 positive areas while increasing ABCA1 expression in the aortic sinus.
体外研究:
E1231(0.1-10 μM;18 小时)促进 RAW 264.7 细胞中的胆固醇流出并抑制脂质积累。 E1231(10 μM;6 小时)显着增加 HepG2 细胞中 Doxo 诱导的 p53 的去乙酰化。