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.