E1231

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

E1231 (E-1231) 是一种小分子 SIRT1 激活剂，EC50 为 0.83 uM。

E1231 (E-1231) is a small molecule SIRT1 activator with EC50 of 0.83 uM, interactes with recombinant human SIRT1 protein and deacetylated liver X receptor-alpha (LXRα); increases ATP-binding cassette transporter A1 (ABCA1) expression in RAW 264.7?cells dependent on SIRT1 and LXRα, promotes cholesterol efflux and inhibited lipid accumulation in RAW 264.7?cells via SIRT1 and ABCA1; decreases total cholesterol and triglyceride levels in both serum and the liver in golden hamster hyperlipidemia models.

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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-/- miceDosage: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.

E-1231

Chromatin/Epigenetic

Sirtuin

Sirtuin

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1031195-19-3

363.417

C21H21N3O3

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (275.17 mM)

CC(N1CCN(C(C2=CC(C3=CC=C(C)O3)=NC4=CC=CC=C24)=O)CC1)=O

1-(4-(2-(5-methylfuran-2-yl)quinoline-4-carbonyl)piperazin-1-yl)ethan-1-one

(-20℃)

With Ice Pack

≥ 2 years