SR9238

SKU: orb1307727

Description

SR9238 is a potent synthetic agonist selective for Liver X Receptors, demonstrating higher affinity for the LXRβ subtype (IC50 = 43 nM) than for LXRα (IC50 = 214 nM). This small molecule is a valuable research tool for studying LXR-mediated pathways in lipid metabolism and inflammation in both cellular and animal models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 1416153-62-2
• MW: 595.73
• Purity: 99.19%
• Formula: C₃₁H₃₃NO₇S₂
• SMILES: CCOC(=O)c1ccc(CN(Cc2ccc(cc2)-c2cccc(c2)S(C)(=O)=O)S(=O)(=O)c2c(C)cc(C)cc2C)o1
• Target: Liver X Receptor
• Solubility: DMSO:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  LXRα:214 nM|LXRβ:43 nM
• In Vivo:
  SR9238 treatment inhibits diet-induced hepatosteatosis, hepatic inflammation, and hepatocellular injury. SR9238 is also detected in the intestine with either i.p. or oral administration. Approximately SR9238 (6 μM) is detected in the liver 2h after the injection of SR9238, but no compound is detected in the plasma. SR9238-treated mice show greatly reduced lipid content in the liver. Both Tnfa and Il1b expression are substantially reduced (~80% and >95%, respectively) in the SR9238-treated mice when compared to the vehicle-treated mice. SR9238-treated DIO mice display a considerably lower intensity of F4/80 staining versus vehicle-treated DIO mice consistent with a beneficial effect of SR9238 on non-alcoholic steatohepatitis. SR9238 treatment does not alter body weight or percent body fat composition relative to vehicle-treated animals during the experiment .
• In Vitro:
  SR9238 effectively suppresses transcription from a fatty acid synthase promoter-driven luciferase reporter. SR9238 is a synthetic LXR inverse agonist (IC50s: 214 nM and 43 nM for LXRα and LXRβ, respectively). SR9238-induced recruitment of CoRNR box peptides is dose-dependent for both LXRα and LXRβ. It is found that SR9238 induces increased interaction of CoRNR box peptides derived from NCoR with both LXRα and LXRβ while causing decreased interaction with a coactivator NR box peptide derived from TRAP220. HepG2 cells treated with SR9238 cause a significant decrease in Fasn and Srebp1c mRNA expression.

Storage & Handling

• Storage: store at low temperature | 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

inhibit, LXRβ, LXRα, LXR, Liver X Receptor, Liver X receptor, LiverXReceptor, Inhibitor, SR 9238, SR9238, SR-9238

Compound Identifiers

PubChem CID

71478195