E1231

E1231 is an orally active activator of Sirtuin 1 ( SIRT1 ) ( EC 50 =0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (K D =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

In Vitro

E1231 (0.1-10 μM; 18 h) promotes cholesterol efflux and inhibits lipid accumulation in RAW 264.7 cells. E1231 (10 μM; 6 h) significantly increases deacetylation of Doxo-induced p53 in HepG2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

E1231 (40 mg/kg; po; once daily for 7 days) regulates cholesterol and lipid metabolism in Golden hamsters fed with HFD diet . E1231 (25, 50, and 100 mg/kg, in 0.5% CMC-Na; po; once daily for 12 weeks) reduces atherosclerosis development, without hepatotoxicity ornephrotoxicity in ApoE -/- mice fed with atherogenic diet . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

Form:Solid

IC50& Target:SIRT1 0.83 μM (EC 50 )