GW6471

Catalog No.S2798 Batch:S279802

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Technical Data

Formula

C35H36F3N3O4
Molecular Weight 619.67 CAS No. 880635-03-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (161.37 mM)
Ethanol 20 mg/mL (32.27 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
Targets
PPARα [1]
(Cell-free assay)
0.24 μM
In vitro

GW6471 completely inhibits GW409544-induced activation of PPARα with IC50 of 0.24 μM. GW6471 at concentration ranging from 0.001-10 μM disrupts the interactions between PPAR and coactivator motifs derived from SRC-1 or CBP, but promotes the binding of the co-repressor motifs from SMRT or N-CoR. GW6471 adopts a U-shaped configuration and wraps around C276 of helix 3, destroys the integrity of the charge clamp but leaves sufficient space to accommodate the additional helical turn of the co-repressor motif in the PPAR/GW6471/SMRT complexes. [1]

GW6471 at concentration of 10 μM significantly prevents cardiomyocyte differentiation and results in the reduced expression of cardiac sarcomeric proteins (ie α-actinin, troponin-T) and specific genes (ie α-MHC, MLC2v) in a time-dependent manner through inhibiting PPARα. [2]
In vivo

GW6471 is a potent PPARα antagonist.

Protocol (from reference)

Kinase Assay:

[1]
  • Binding assays

    The effects of GW6471 on the interaction of coactivator and co-repressor peptides with PPAR are determined by chemical-mediated fluorescence energy transfer assays. The experiments are conducted with 5 nM PPARα LBD of biotinylated peptide containing individual motifs , following the manufacturer
Animal Study:

[5]
  • Animal Models

    Male athymic Nu/Nu mice

  • Dosages

    20 mg/kg

  • Administration

    i.p.

Selleck's GW6471 has been cited by 20 publications

CD24 negativity reprograms mitochondrial metabolism to PPARα and NF-κB-driven fatty acid β-oxidation in triple-negative breast cancer [ Cancer Lett, 2024, 587:216724] PubMed: 38373689
Tubular CPT1A deletion minimally affects aging and chronic kidney injury [ JCI Insight, 2024, 9(6)e171961] PubMed: 38516886
PIM1 drives lipid droplet accumulation to promote proliferation and survival in prostate cancer [ Oncogene, 2024, 43(6):406-419] PubMed: 38097734
Astragaloside IV ameliorates cisplatin-induced liver injury by modulating ferroptosis-dependent pathways [ J Ethnopharmacol, 2024, 328:118080] PubMed: 38521426
Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis [ Nat Commun, 2023, 14(1):6908] PubMed: 37903763
Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis [ Nat Commun, 2023, 14(1):6908] PubMed: 37903763
Suppression of the gut microbiota-bile acid-FGF19 axis in patients with atrial fibrillation [ Cell Prolif, 2023, e13488.] PubMed: 37186335
RAE1 promotes nitrosamine-induced malignant transformation of human esophageal epithelial cells through PPARα-mediated lipid metabolism [ Ecotoxicol Environ Saf, 2023, 265:115513] PubMed: 37774541
Protective effect of Saussurea involucrata polysaccharide against skin dryness induced by ultraviolet radiation [ Front Pharmacol, 2023, 14:1089537] PubMed: 36733502
3β-Hydroxy-12-oleanen-27-oic Acid Exerts an Antiproliferative Effect on Human Colon Carcinoma HCT116 Cells via Targeting FDFT1 [ Int J Mol Sci, 2023, 10.3390/ijms241915020] PubMed: 37834468

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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