GW 6471

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Cat.No. 4618 - GW 6471 | C35H36F3N3O4 | CAS No. 880635-03-0
Description: PPARα antagonist
Chemical Name: N-((2S)-2-(((1Z)-1-Methyl-3-oxo-3-(4-(trifluoromethyl)phenyl)prop-1-enyl)amino)-3-(4-(2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy)phenyl)propyl)propanamide
Purity: ≥98% (HPLC)
Citations (13)

Biological Activity

PPARα antagonist (IC50 = 0.24 μM). Enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.

Licensing Information

Sold with the permission of GlaxoSmithKline.

Compound Libraries

GW 6471 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 619.67
Formula C35H36F3N3O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 880635-03-0
PubChem ID 446738
Smiles CC2=C(N=C(C4=CC=CC=C4)O2)CCOC(C=C1)=CC=C1C[C@@H](CNC(CC)=O)N/C(C)=C\C(C3=CC=C(C(F)(F)F)C=C3)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 46.48 75
ethanol 12.39 20

Preparing Stock Solutions

The following data is based on the product molecular weight 619.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.61 mL 8.07 mL 16.14 mL
5 mM 0.32 mL 1.61 mL 3.23 mL
10 mM 0.16 mL 0.81 mL 1.61 mL
50 mM 0.03 mL 0.16 mL 0.32 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

Xu et al (2002) Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα. Nature 415 813 PMID: 11845213

Muller et al (2009) An innovative method to study target protein-drug interactions by mass spectrometry. J.Med.Chem. 52 2875 PMID: 19379014

If you know of a relevant reference for GW 6471, please let us know.

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Keywords: GW 6471, supplier, GW6471, PPAR, PPARa, PPARalpha, PPARα, peroxisome, proliferator-activated, receptor, alpha, antagonists, GlaxoSmithKline, gsk, PPARalpha, Receptors, PPARalpha, Receptors, Tocris Bioscience

13 Citations for GW 6471

Citations are publications that use Tocris products. Selected citations for GW 6471 include:

Kok et al (2013) Differential regulation of the expressions of the PGC-1α splice variants, lipins, and PPARα in heart compared to liver. J Lipid Res 54 1662 PMID: 23505321

Crane et al (2013) Lipids derived from virulent Francisella tularensis broadly inhibit pulmonary inflammation via toll-like receptor 2 and peroxisome proliferator-activated receptor α. Clin Vaccine Immunol 20 1531 PMID: 23925884

El-Sisi et al (2013) Effects of three different fibrates on intrahepatic cholestasis experimentally induced in rats. J Neuroinflammation 2013 781348 PMID: 23997763

Bumpus and Johnson (2011) 5-Aminoimidazole-4-carboxyamide-ribonucleoside (AICAR)-stimulated hepatic expression of Cyp4a10, Cyp4a14, Cyp4a31, and other peroxisome proliferator-activated receptor α-responsive mouse genes is AICAR 5'-monophosphate-dependent and AMP-activated Br J Pharmacol 339 886 PMID: 21896918

Carracedo et al (2012) A metabolic prosurvival role for PML in breast cancer. J Clin Invest 122 3088 PMID: 22886304

Oruqaj et al (2015) Compromised peroxisomes in idiopathic pulmonary fibrosis, a vicious cycle inducing a higher fibrotic response via TGF-β signaling. Proc Natl Acad Sci U S A 112 E2048 PMID: 25848047

Qian et al (2015) Peroxisomes in Different Skeletal Cell Types during Intramembranous and Endochondral Ossification and Their Regulation during Osteoblast Differentiation by Distinct Peroxisome Proliferator-Activated Receptors. PLoS One 10 e0143439 PMID: 26630504

Lin et al (2015) Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. J Appl Toxicol 16 5555 PMID: 25768340

Midgett et al (2015) In vitro evaluation of the effects of perfluorooctanesulfonic acid (PFOS) and perfluorooctanoic acid (PFOA) on IL-2 production in human T-cells. J Pharmacol Exp Ther 35 459 PMID: 25056757

Borrelli et al (2015) Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. Lipids Health Dis 172 142 PMID: 25205418

Redlich et al (2014) Palmitoylethanolamide stimulates phagocytosis of Escherichia coli K1 by macrophages and increases the resistance of mice against infections. Int J Mol Sci 11 108 PMID: 24927796

Kong et al (2012) Activation of peroxisome proliferator activated receptor α ameliorates ethanol induced steatohepatitis in mice. PPAR Res 10 246 PMID: 22208561

Mottillo et al (2012) Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. J Neuroinflammation 287 25038 PMID: 22685301

Do you know of a great paper that uses GW 6471 from Tocris? If so please let us know.

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