2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
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  4. GW6471

GW6471 is a potent PPARα antagonist.

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

GW6471 Chemical Structure

GW6471 Chemical Structure

CAS No. : 880635-03-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
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5 mg USD 60 In-stock
10 mg USD 100 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
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Customer Review

Based on 48 publication(s) in Google Scholar

GW6471 Related Antibodies

Top Publications Citing Use of Products

45 Publications Citing Use of MCE GW6471

IF
RT-PCR
WB

    GW6471 purchased from MedChemExpress. Usage Cited in: J Dairy Sci. 2023 Feb 14;S0022-0302(23)00052-8.  [Abstract]

    GW6471 significantly reduces the regulatory effects of GINY and DQW on the protein expression levels of PPARα, CPT-1a, ACOX1, HO-1, and FASN in HepG2 cells.

    GW6471 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3;2019:7536803.  [Abstract]

    The antihypertrophic effects of zileuton ar counteracted by GW6471 as indicated by increased PE-induced hypertrophic marker transcription, cell surface area, and oxidative stress when compared with those in the PE group and PE+ zileuton group.

    GW6471 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2019 Nov 3;2019:7536803.  [Abstract]

    Cells are treated with PE (50 μM), zileuton (100 μM), and GW6471 (10 μM) for 24 h. α-Actinin staining (n = 6) results in H9c2 cells.

    View All PPAR Isoform Specific Products:

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    PPARα PPARβ/δ PPARγ PPAR PPARδ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GW6471 is a potent PPARα antagonist.

    IC50 & Target[1]

    PPARα

     

    In Vitro

    In a cell-based reporter assay, GW6471 completely inhibits GW409544-induced activation of PPARα with an IC50 of 0.24 μM[1]. The functional role of PPARα is evaluated on renal cell carcinoma (RCC) cell viability by MTT assay. Both Caki-1 (VHL wild type) and 786-O (VHL mutated) cells are incubated separately with a specific PPARα agonist, WY14,643, or a specific PPARα antagonist, GW6471 at concentrations from 12.5 to 100 μM for 72 hours, and cell viability is assessed. While WY14,643 either has no affect on, or slightly increased, cell viability, GW6471 significantly and dose-dependently inhibits cell viability (up to approximately 80%) in both cell lines[2].

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

    GW6471 Related Antibodies
    In Vivo

    To test the antitumor activity of PPARα antagonism in vivo, a subcutaneous xenograft mouse model is used. Caki-1 cells are implanted subcutaneously in nude (Nu/Nu) mice. After tumor masses reach ～5 mm in diameter, GW6471 is administrated intraperitoneally every other day for 4 wk at a dose (20 mg/kg mouse body wt) that is described to be effective in an in vivo dose-response study and confirmed here to be efficacious. There are significant differences in tumor growth between vehicle- and GW6471-treated animals. No toxicity is observed at the doses of GW6471 based on weights of the animals, and laboratory values, including kidney and liver function tests, are not adversely affected. To demonstrate on-target effects of GW6471, c-Myc levels are evaluated in the tumors, which show significant decreases in the GW6471-treated animals[3].

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

    619.67

    Formula

    C35H36F3N3O4
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    CCC(NC[C@@H](N/C(C)=C\C(C1=CC=C(C(F)(F)F)C=C1)=O)CC2=CC=C(OCCC3=C(C)OC(C4=CC=CC=C4)=N3)C=C2)=O
    Shipping

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

    DMSO : 83.33 mg/mL (134.47 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6138 mL 8.0688 mL 16.1376 mL
    5 mM 0.3228 mL 1.6138 mL 3.2275 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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

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    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: ≥ 2.08 mg/mL (3.36 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (3.36 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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: 99.64%

    SDS (393 KB)

    COA (247 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    786-O and Caki-1 cells are plated in 96 well plates. Both cells are incubated separately with WY14,643 or GW 6471 at concentrations from 12.5 to 100 µM for 72 hours, and after the indicated treatments, the cells are incubated in MTT solution/media mixture. Then, the MTT solution is removed and the blue crystalline precipitate in each well is dissolved in DMSO. Visible absorbance of each well at 540 nm is quantified using a microplate reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3]

    Mice[3]
    Male athymic Nu/Nu mice (8 wk of age, ~25 g body wt) are injected with 1×105 Caki-1 cells subcutaneously (3:1 DMEM-Matrigel) in the flank region. Tumor progression is monitored weekly by calipers. When tumor size reaches ~80-100 mm3, animals are randomly assigned to four groups and treatments are started (day 1). The vehicle group receive DMSO (4% in PBS) intraperitoneally and vegetable oil via oral gavage. The PPARα group is injected intraperitoneally with GW 6471 in the same vehicle (20 mg/kg body wt; murine dose response is reported elsewhere) every other day. The Sunitinib group receive Sunitinib in vegetable oil via oral gavage (40 mg/kg body wt) 5 days/wk. Another group receive GW 6471+Sunitinib. To determine any potential toxicity of the treatment(s), body weights of the animals are measured and signs of adverse reactions are monitored. On day 28, the mice are euthanized and the tumor mass is determined. Tumor growth rate is calculated[3].

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6138 mL 8.0688 mL 16.1376 mL 40.3441 mL
    5 mM 0.3228 mL 1.6138 mL 3.2275 mL 8.0688 mL
    10 mM 0.1614 mL 0.8069 mL 1.6138 mL 4.0344 mL
    15 mM 0.1076 mL 0.5379 mL 1.0758 mL 2.6896 mL
    20 mM 0.0807 mL 0.4034 mL 0.8069 mL 2.0172 mL
    25 mM 0.0646 mL 0.3228 mL 0.6455 mL 1.6138 mL
    30 mM 0.0538 mL 0.2690 mL 0.5379 mL 1.3448 mL
    40 mM 0.0403 mL 0.2017 mL 0.4034 mL 1.0086 mL
    50 mM 0.0323 mL 0.1614 mL 0.3228 mL 0.8069 mL
    60 mM 0.0269 mL 0.1345 mL 0.2690 mL 0.6724 mL
    80 mM 0.0202 mL 0.1009 mL 0.2017 mL 0.5043 mL
    100 mM 0.0161 mL 0.0807 mL 0.1614 mL 0.4034 mL
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    GW6471 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:

    GW6471880635-03-0GW 6471GW-6471PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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