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 |
| 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)=CC(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 | |
|---|---|---|---|
| Solubility | |||
| 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
References
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
Keywords: GW 6471, supplier, GW6471, PPAR, PPARa, PPARalpha, PPARα, peroxisome, proliferator-activated, receptor, alpha, antagonists, GlaxoSmithKline, gsk, PPARalpha, Receptors, PPARalpha, Receptors, Tocris Bioscience
