| Bioactivity | 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[1]. |
| Invitro | 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[1]。 E1231（10 μM；6 小时）显着增加 HepG2 细胞中 Doxo 诱导的 p53 的去乙酰化[1]。 |
| In Vivo | 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[1]。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[1]。 Animal Model: |
| Name | E1231 |
| CAS | 1031195-19-3 |
| Formula | C21H21N3O3 |
| Molar Mass | 363.41 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Feng T, et al. SIRT1 activator E1231 protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression. Atherosclerosis. 2018 Jul;274:172-181. |