1. Metabolic Enzyme/Protease
  2. FXR

GW 4064 

Cat. No.: HY-50108 Purity: 99.42%
Handling Instructions

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

For research use only. We do not sell to patients.

GW 4064 Chemical Structure

GW 4064 Chemical Structure

CAS No. : 278779-30-9

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 72 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 96 In-stock
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50 mg USD 300 In-stock
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100 mg USD 540 In-stock
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200 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
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1 g   Get quote  

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Customer Review

    GW 4064 purchased from MCE. Usage Cited in: FEBS Lett. 2017 Sep;591(18):2836-2847.

    GW4064 inhibits NLRP3 inflammasome activation. The human PBMCs are primed with 500 ng/mL LPS for 3 h followed by GW4064 of indicated concentration(s) and different second signal stimulations, including Nigericin. The protein levels of activated caspase-1 and cleaved IL-1b are detected by western blot.

    GW 4064 purchased from MCE. Usage Cited in: Int J Mol Sci. 2018 Jun 28;19(7). pii: E1898.

    Western blotting for p-FAK and total FAK. Cells are treated with vehicle control (Cont), 10 μM GW4064, or 32 μM GS in the absence or presence of 10 ng/mL TGF-β for 48 h. .

    GW 4064 purchased from MCE. Usage Cited in: FASEB J. 2018 Oct 11:fj201801181R.

    FXRa protein expression in nontransduced (treated with DMSO or GW4064 for 9 d) and transduced shFXRa-dHepaRG cells, by Western blot analysis.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    EC50: 65 nM (FXR)[1]

    In Vitro

    Treatment with different concentrations of GW4064 (1, 2.5, 5, 10 μM) reduces the lipid accumulation in the cells. Concordantly, GW4064 treatment significantly represses oleic acid-induced CD36 protein levels in a dose-dependent manner. Taken together, these data indicate that prevention of hepatic lipid accumulation is likely due to an inhibition of Cd36 expression by long-term GW4064 treatment[2].

    In Vivo

    GW4064 suppresses weight gain in C57BL/6 mice fed with either a high-fat diet (HFD) or high-fat, high-cholesterol diet. GW4064 treatment of mice on HFD significantly represses diet-induced hepatic steatosis as evidenced by lower triglyceride and free fatty acid level in the liver. GW4064 markedly reduces lipid transporter CD36 expression without affecting expression of genes that are directly involved in lipogenesis. GW4064 treatment attenuates hepatic inflammation while having no effect on white adipose tissue[2]. GW4064 (30 mg/kg) treatment results in substantial, statistically significant reductions in serum activities of ALT, AST, LDH, and ALP in the ANIT-treated rats. Serum bile acid levels are also significantly reduced by GW4064 treatment. Bilirubin levels are decreased in the GW4064-treated rats, but statistical significance is not achieved. Notably, GW4064 is much more effective in decreasing these markers of liver damage than TUDCA, which reduces only LDH levels[3].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 150 mg/mL (276.32 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8422 mL 9.2108 mL 18.4216 mL
    5 mM 0.3684 mL 1.8422 mL 3.6843 mL
    10 mM 0.1842 mL 0.9211 mL 1.8422 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Cell Assay
    [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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    Mice[2]
    Fifteen-week-old male C57BL/6 mice are fed a high-fat diet with or without additional 0.2% Cholesterol and received twice weekly injections of GW 4064 (50 mg/kg, intra-peritoneal) or carrier solution (DMSO) solution for 6 weeks. Animals are weighed weekly and their body composition is determined using EchoMRI-100TM from Echo Medical Systems.
    Rats[3]
    Animals. Adult male CRL:CD(SD)IGS rats weighing 300-350 g, are used. The rats receive a single analgesic dose of oxymorphone following surgery. Twenty-four hours after laparotomy, groups of rats (n=6) receive intraperitoneal injections once daily for 4 days. Bile duct-ligated (BDL) rats are treated with 5 mL/kg corn oil as vehicle, 30 mg/kg GW4064 in corn oil, or 15 mg/kg TUDCA in corn oil. Sham-operated animals received 5 mL/kg corn oil vehicle. Four hours after the final dose, serum and livers are collected for analysis.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    542.84

    Formula

    C₂₈H₂₂Cl₃NO₄

    CAS No.

    278779-30-9

    SMILES

    O=C(C1=CC=CC(/C=C/C2=CC=C(C=C2Cl)OCC3=C(ON=C3C4=C(Cl)C=CC=C4Cl)C(C)C)=C1)O

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.42%

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    Product Name:
    GW 4064
    Cat. No.:
    HY-50108
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    GW 4064

    Cat. No.: HY-50108