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GW4064
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GW4064图片
CAS NO:278779-30-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)542.84
FormulaC28H22Cl3NO4
CAS No.278779-30-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 100 mg/mL (184.2 mM)
Water: <1 mg/mL
Ethanol:<1 mg/mL
Solubility (In vivo)0.5% methylcellulose: 11 mg/mL
SynonymsGW-4064; GW4064; GW 4064
实验参考方法
In Vitro

In vitro activity: GW 4064 is a full agonist with EC50 values of 80 and 90 nM, respectively, in CV-1 cells transfected with mouse and human FXR expression vectors and an established reporter gene. There is no activity of GW 4064 on other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. Thus, GW 4064 is a potent and selective nonsteroidal FXR agonist.


Kinase Assay: GW 4064 is a potent FXR agonist with EC50 of 65 nM.


Cell Assay: 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.

In VivoPharmacokinetic analysis in rats shows that GW 4064 possesses an oral bioavailability of 10% with a t1/2 = 3.5 h. Fisher rats are dosed with GW 4064 by oral gavage. After 7 days, a dose-dependent lowering of serum triglycerides is observed in the rats receiving GW 4064, with an ED50 = 20 mg/kg.
Animal modelFisher rats
Formulation & DosageDissolved in 0.5% methyl cellulose; 0-100 mg/kg; Oral gavage
ReferencesBioorg Med Chem Lett. 2008 Aug 1;18(15):4339-43; J Med Chem. 2000 Aug 10;43(16):2971-4.