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  3. GW6471

GW6471 

Cat. No.: HY-15372 Purity: 98.71%
COA Handling Instructions

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

Size Price Stock Quantity
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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
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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500 mg   Get quote  

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Customer Review

Based on 39 publication(s) in Google Scholar

Top Publications Citing Use of Products

36 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]

    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.

    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.

    View All PPAR Isoform Specific Products:

    • 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.

    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

    Light yellow 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)

    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
    10 mM 0.1614 mL 0.8069 mL 1.6138 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 98.81%

    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
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    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.

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    Product Name:
    GW6471
    Cat. No.:
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