GW 6471

Name: GW 6471
Brand: Tocris Bioscience
SKU: 4618

Tocris Bioscience, part of Bio-Techne | Catalog # 4618

Citations (118)

COA / SDS

PPARα antagonist

Key Product Details

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)
Molecular Weight:	619.67

View Full Technical Details for GW 6471

Technical Data
Citations

Biological Activity for GW 6471

GW 6471 is a PPARα antagonist (IC₅₀ = 0.24 μM). GW 6471 enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR. GW 6471 blocks SARS-CoV-2 infection in airway organoids (EC₅₀ = 2.1 μM) by blocking and downregulating the hypoxia inducible factor 1 subunit alpha (HIF1α) and HIF1 pathway; also reduces viral RNA. GW 6471 induces apoptosis and cell cycle arrest in kidney cancer cells.

Licensing Information

Sold with the permission of GlaxoSmithKline.

Compound Libraries for GW 6471

GW 6471 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GW 6471

M. Wt	619.67
Formula	C₃₅H₃₆F₃N₃O₄
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	880635-03-0
PubChem ID	446738
InChi Key	TYEFSRMOUXWTDN-DYQICHDWSA-N
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GW 6471

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	46.48	75
	ethanol	6.2	10

Preparing Stock Solutions for GW 6471

The following data is based on the product molecular weight 619.67.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.75 mM	2.15 mL	10.76 mL	21.52 mL
3.75 mM	0.43 mL	2.15 mL	4.30 mL
7.5 mM	0.22 mL	1.08 mL	2.15 mL
37.5 mM	0.04 mL	0.22 mL	0.43 mL

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References for GW 6471

References are publications that support the biological activity of the product.

Aboud Inhibition of PPARα induces cell cycle arrest and apoptosis, and synergizes with glycolysis inhibition in kidney cancer cells. PLoS One 2013 PMID: 23951092
Muller An innovative method to study target protein-drug interactions by mass spectrometry. J.Med.Chem. 2009 PMID: 19379014
Duan An airway organoid-based screen identifies a role for the HIF1α-glycolysis axis in SARS-CoV-2 infection. Cell Rep. 2021 PMID: 34731648
Xu Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα. Nature 2002 PMID: 11845213