GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).

FXR:65 nM(EC50)

In Fisher rats, oral administration of GW 4064 (ED50 = 20 mg/kg) effectively reduces serum triglycerides.

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.

GW 4064 is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. 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[2].