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    InvivoChem Cat #: V1841
    CAS #: 278779-30-9Purity ≥98%

    Description: GW4064 is a novel, potent and selective agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line. It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM. GW-4064 upregulates adipokine expression in preadipocytes and HepG2 cells. GW4064 could reduce induction of proinflammatory cytokines by LPS in vitro. GW4064 shows beneficial effects on cholesterol and TG (triglycerides) in various animal species. GW4064 is found to lower serum TG levels in both the KK-Ay and ob/ob mice potently. In KK-Ay mice, a 1-week administration of GW4064 also significantly lowers VLDL secretion. GW4064 can also lower serum TGs in the SHP+/+ mice.

    References: Bioorg Med Chem Lett. 2008 Aug 1;18(15):4339-43; J Med Chem. 2000 Aug 10;43(16):2971-4.

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    Molecular Weight (MW)542.84
    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
    SynonymsGW4064; GW-4064; GW 4064

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    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.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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