E1231

SKU: orb1298365

Description

E1231 is a SIRT1-activating small molecule that upregulates ABCA1 expression. It demonstrates anti-atherosclerotic effects in experimental models, reducing plasma cholesterol and triglyceride levels, making it a valuable research tool for cardiovascular and metabolic disease studies.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1031195-19-3
• MW: 363.41
• Purity: 98.86%
• Formula: C₂₁H₂₁N₃O₃
• SMILES: C(=O)(C=1C2=C(N=C(C1)C=3OC(C)=CC3)C=CC=C2)N4CCN(C(C)=O)CC4
• Target: Sirtuin
• Solubility: DMSO:60 mg/mL (165.1 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.5 mM)

Bioactivity

• Target IC50:
  SIRT1:0.83 μM (EC50)
• 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.
• 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

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SIRT1, E1231, E-1231, E 1231

Compound Identifiers

PubChem CID

24980435