1. Cell Cycle/DNA Damage
  2. PPAR
  3. GW 6471

GW 6471 

Cat. No.: HY-15372 Purity: 98.98%
Handling Instructions

GW 6471 is a potent PPARα antagonist.

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

GW 6471 Chemical Structure

GW 6471 Chemical Structure

CAS No. : 880635-03-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 204 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 220 In-stock
Estimated Time of Arrival: December 31
50 mg USD 880 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GW 6471 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2019 Oct. 

    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.

    GW 6471 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2019 Oct. 

    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

    GW 6471 is a potent PPARα antagonist.

    IC50 & Target[1]

    PPARα

     

    In Vitro

    In a cell-based reporter assay, GW 6471 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, GW 6471 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, GW 6471 significantly and dose-dependently inhibits cell viability (up to approximately 80%) in both cell lines[2].

    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, GW 6471 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 GW 6471-treated animals. No toxicity is observed at the doses of GW 6471 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 GW 6471, c-Myc levels are evaluated in the tumors, which show significant decreases in the GW 6471-treated animals[3].

    Molecular Weight

    619.67

    Formula

    C₃₅H₃₆F₃N₃O₄

    CAS No.

    880635-03-0

    SMILES

    CCC(NC[[email protected]@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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (201.72 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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% corn oil

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

    *All of the co-solvents are provided by MCE.
    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
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    GW 6471GW6471GW-6471PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product name:
    GW 6471
    Cat. No.:
    HY-15372
    Quantity:
    MCE Japan Authorized Agent: