2. Metabolic Enzyme/Protease Autophagy
  3. FXR Autophagy
  4. GW 4064

GW 4064 is a potent FXR agonist with an 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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 In-stock
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10 mM * 1 mL in DMSO USD 72 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 96 In-stock
50 mg USD 300 In-stock
100 mg USD 540 In-stock
200 mg USD 1020 In-stock
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Customer Review

Based on 41 publication(s) in Google Scholar

Other Forms of GW 4064:

GW 4064 Related Antibodies

Top Publications Citing Use of Products

36 Publications Citing Use of MCE GW 4064

WB
RT-PCR

    GW 4064 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2019 Dec 13;17(1):418.  [Abstract]

    FXR suppresses gluconeogenesis and enhances glucose uptake in the HK-2 cell lines. The protein expression of FXR is obviously upregulates by GW4064 at 24, 48 and 72 h in the HK-2 cell lines.

    GW 4064 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2019 Dec 13;17(1):418.  [Abstract]

    FXR suppresses gluconeogenesis and enhances glucose uptake in the HK-2 cell lines. GW4064 at 4 μM inhibits the mRNA level of FXR.

    GW 4064 purchased from MedChemExpress. Usage Cited in: FASEB J. 2019 Feb;33(2):2472-2483.  [Abstract]

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

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

    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 MedChemExpress. Usage Cited in: FEBS Lett. 2017 Sep;591(18):2836-2847.  [Abstract]

    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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GW 4064 is a potent FXR agonist with an 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].

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

    GW 4064 Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    542.84

    Formula

    C28H22Cl3NO4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (184.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    DMF : 100 mg/mL (184.22 mM; Need ultrasonic)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMF    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 5 mg/mL (9.21 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC/saline water

      Solubility: 5 mg/mL (9.21 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.61%

    SDS (393 KB)

    COA (252 KB) HNMR (277 KB) RP-HPLC (223 KB) LCMS (87 KB) Elemental Analysis Report (110 KB)

    Handling Instructions (2659 KB)
    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). 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. 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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / DMF 1 mM 1.8422 mL 9.2108 mL 18.4216 mL 46.0541 mL
    5 mM 0.3684 mL 1.8422 mL 3.6843 mL 9.2108 mL
    10 mM 0.1842 mL 0.9211 mL 1.8422 mL 4.6054 mL
    15 mM 0.1228 mL 0.6141 mL 1.2281 mL 3.0703 mL
    20 mM 0.0921 mL 0.4605 mL 0.9211 mL 2.3027 mL
    25 mM 0.0737 mL 0.3684 mL 0.7369 mL 1.8422 mL
    30 mM 0.0614 mL 0.3070 mL 0.6141 mL 1.5351 mL
    40 mM 0.0461 mL 0.2303 mL 0.4605 mL 1.1514 mL
    50 mM 0.0368 mL 0.1842 mL 0.3684 mL 0.9211 mL
    60 mM 0.0307 mL 0.1535 mL 0.3070 mL 0.7676 mL
    80 mM 0.0230 mL 0.1151 mL 0.2303 mL 0.5757 mL
    100 mM 0.0184 mL 0.0921 mL 0.1842 mL 0.4605 mL
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    GW 4064 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    GW 4064278779-30-9GW4064GW-4064FXRAutophagyNR1H4Inhibitorinhibitorinhibit

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