1. Cell Cycle/DNA Damage
  2. PPAR

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

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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
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100 mg USD 1550 In-stock
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View All PPAR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

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    90% corn oil

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

  • 2.

    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

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
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

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

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GW 6471
Cat. No.:
HY-15372
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GW 6471

Cat. No.: HY-15372