A potent, selective agonist of farnesoid X receptor
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GW 4064

Item No. 10006611

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-benzoic acid
CAS Number
278779-30-9
Molecular Formula
C28H22Cl3NO4
Formula Weight
542.8
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 25 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/mlEthanol: 1 mg/ml
λmax
304 nm
SMILES
ClC(C=CC=C1Cl)=C1C2=NOC(C(C)C)=C2COC(C=C3)=CC(Cl)=C3/C=C/C4=CC(C(O)=O)=CC=C4
InChi Code
InChI=1S/C28H22Cl3NO4/c1-16(2)27-21(26(32-36-27)25-22(29)7-4-8-23(25)30)15-35-20-12-11-18(24(31)14-20)10-9-17-5-3-6-19(13-17)28(33)34/h3-14,16H,15H2,1-2H3,(H,33,34)/b10-9+
InChi Key
BYTNEISLBIENSA-MDZDMXLPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $36

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    5 mg

    $95

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    10 mg

    $147

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    Cayman Chemical
    Explore Obesity & Metabolic Disease Resources

    Discover high-quality research tools to investigate GLP-1 mechanisms and next-generation metabolic targets.

    OBESITY RESEARCH SOLUTIONS
    Product Description

    GW 4064 is a selective agonist of FXR (EC50 = 15 nM).1 It displays no activity at other nuclear receptors, including the retinoic acid receptor, at concentrations up to 1 μM.1 GW 4064 is used to elucidate the role of FXR in dyslipidemia, diabetes, obesity, and cancer.2,3,4,5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maloney, P.R., Parks, D.J., Haffner, C.D., et al. Identification of a chemical tool for the orphan nuclear receptor FXR. J. Med. Chem. 43(16), 2971-2974 (2000).

    2. Haeusler, R.A., Pratt-Hyatt, M., Welch, C.L., et al. Impaired generation of 12-hydroxylated bile acids links hepatic insulin signaling with dyslipidemia. Cell Metab. 15(1), 65-74 (2012).

    3. Watanabe, M., Horai, Y., Houten, S.M., et al. Lowering bile acid pool size with a synthetic farnesoid X receptor (FXR) agonist induces obesity and diabetes through reduced energy expenditure. The Journal of Biological Chemisty 286(30), 26913-26920 (2011).

    4. Deuschle, U., Schüler, J., Schulz, A., et al. FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model. PLoS One 7(10), e43044 (2012).

    5. Catalano, S., Malvindi, R., Giordano, C., et al. Farnesoid X receptor, through the binding with steroidogenic factor 1-responsive element, inhibits aromatase expression in tumor Leydig cells. The Journal of Biological Chemisty 285(8), 5581-5593 (2010).

    6. Cariou, B., van Harmelen, K., Duran-Sandoval, D., et al. The farnesoid X receptor modulates adiposity and peripheral insulin sensitivity in mice. The Journal of Biological Chemisty 281(16), 11039-11049 (2006).