GW 4064

SKU: orb1305997

Description

GW 4064 is a potent and selective synthetic agonist of the farnesoid X receptor (FXR), exhibiting an EC50 of 65 nM. This tool compound is widely used in both in vitro and in vivo research to investigate FXR's role in bile acid homeostasis, metabolic disorders, and liver diseases.

Research Area

Cell Biology, Metabolism Research

Key Properties

• CAS Number: 278779-30-9
• MW: 542.84
• Purity: 99.94% (May vary between batches)
• Formula: C₂₈H₂₂Cl₃NO₄
• SMILES: CC(C)c1onc(c1COc1ccc(C=Cc2cccc(c2)C(O)=O)c(Cl)c1)-c1c(Cl)cccc1Cl
• Target: FXR,Autophagy
• Solubility: DMSO:50 mg/mL (92.11 mM);Ethanol:5.4 mg/mL (9.95 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.68 mM)

Bioactivity

• Target IC50:
  FXR:65 nM(EC50)
• In Vivo:
  In CV-1 cells transfected with mouse FXR expression vectors (EC50=80 nM) and in CV-1 cells transfected with human FXR expression vectors (EC50=90 nM), GW 4064 functions as a selective non-steroidal FXR agonist, effectively exerting agonistic effects.
• In Vitro:
  In Fisher rats, oral administration of GW 4064 (ED50 = 20 mg/kg) effectively reduces serum triglycerides.
• Cell Research:
  GW 4064 is dissolved in DMSO and stored, and then diluted with appropriate media before use. Mouse liver cells (BNL CL.2) are maintained in a humidified incubator under 5% CO2 at 37°C in Dulbecco's Modified Eagle's Medium (DMEM) supplemented with 10% fetal bovine serum (FBS) and 1% Penicillin/Streptomycin. When cells are divided into six-well plates and reach ~90% confluence, sub-confluent cells are washed three times with phosphate buffered saline (PBS) and replaced with serum-free DMEM supplemented with 1% fatty acid-free BSA. Oleic acid (final concentration 500 μM) and GW4064 at various concentrations are added and incubated for 24 h. Cells are then fixed with 4% formaldehyde for Oil Red O staining or harvested for protein and western blot analysis.

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

Inhibitor, NR1H4, inhibit, GW 4064, GW4064, GW-4064, FXR, Autophagy

Compound Identifiers

PubChem CID

44483281