GW 6471
Tocris Bioscience, part of Bio-Techne | Catalog # 4618
PPARα antagonist
Product Description
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.Product Specifications
Molecular Weight
619.67
Formula
C35H36F3N3O4
Storage
Store at +4°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
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
Product Specific Notices for GW 6471
For research use only
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