| Identification | Back Directory | [Name]
E1231 | [CAS]
1031195-19-3 | [Synonyms]
E1231
1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one | [Molecular Formula]
C21H21N3O3 | [MOL File]
1031195-19-3.mol | [Molecular Weight]
363.41 |
| Chemical Properties | Back Directory | [Boiling point ]
605.8±55.0 °C(Predicted) | [density ]
1.259±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
2.90±0.61(Predicted) | [color ]
Off-white to light brown |
| Hazard Information | Back Directory | [Description]
E1231 is a SIRT1 activator which protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression. | [Uses]
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]. | [in vivo]
E1231 (40 mg/kg; po; once daily for 7 days) regulates cholesterol and lipid metabolism in Golden hamsters fed with HFD diet[1].
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[1].
| Animal Model: | HFD-diet Golden hamsters (80-90 g)[1] | | 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[1] | | 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. |
| [IC 50]
SIRT1: 0.83 μM (EC50) | [References]
[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. DOI:10.1016/j.atherosclerosis.2018.04.039 |
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