GW 4064

FXR:65 nM(EC50)

在小鼠FXR表达载体转染的CV-1细胞中（EC50=80 nM）,在人FXR表达载体转染的CV-1细胞中（EC50=90 nM）,GW 4064作为选择性非甾体FXR激动剂,能够发挥激动作用。

在Fisher大鼠中,口服给药GW 4064（ED50 = 20 mg/kg）,能够降低大鼠血清中的甘油三酯.

DMSO:54.3 mg/mL (100 mM),Ethanol:5.4 mg/mL (10 mM)

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].