| Name | E1231 |
| Description | E1231 is an activator of SIRT1 . E1231 protects from experimental atherosclerosis and lowers plasma cholesterol and triglycerides by enhancing ABCA1 expression. |
| Cell Research | A high-throughput screening assay was established to identify SIRT1 activators. Surface plasmon resonance and immunoprecipitation were performed to confirm the interaction of E1231 with SIRT1. Cholesterol assay was performed to demonstrate the in vitro effect of E1231. The in vivo effect of E1231 was evaluated in experimental models
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| In vitro | E1231, a piperazine 1,4-diamide compound, was identified as a SIRT1 activator with EC50value of 0.83 μM. E1231 interacted with recombinant human SIRT1 protein and deacetylated liver X receptor-alpha (LXRα). E1231 increased ATP-binding cassette transporter A1 (ABCA1) expression in RAW 264.7 cells dependent on SIRT1 and LXRα. E1231 promoted cholesterol efflux and inhibited lipid accumulation in RAW 264.7 cells via SIRT1 and ABCA1. In the golden hamster hyperlipidemia model, E1231 treatment decreased total cholesterol and triglyceride levels in both serum and the liver, while increased cholesterol content in feces. Moreover, E1231 increased ABCA1 and SIRT1 protein expression in the liver. In ApoE-/-?mice, E1231 treatment reduced atherosclerotic plaque development compared with untreated ApoE-/-?mice. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60 mg/mL (165.1 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.5 mM), Sonication is recommended.
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| Keywords | SIRT1 | E-1231 | E1231 | E 1231 |
| Inhibitors Related | JGB1741 | Nicotinamide riboside malate | Sirtinol | Selisistat | MDL-800 | Dihydrocoumarin | SRT 2104 | Nicotinamide riboside | MC3482 | Fisetin | SIRT5 inhibitor 8 | Nicotinamide |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Endoplasmic Reticulum Stress Compound Library | Epigenetics Compound Library | Glutamine Metabolism Compound Library | Antioxidant Compound Library | NO PAINS Compound Library | Mitochondria-Targeted Compound Library | Anti-Cardiovascular Disease Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
