Biological Activity
Selective irreversible PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively). Blocks the inhibition of osteoclast formation induced by IL-4 in the low micromolar range (1-2 μM), therefore is more potent than BADGE (Cat. No. 1326). Anticancer, inhibits growth of human mammary tumor cell lines.
Technical Data
| M. Wt | 276.68 |
| Formula | C13H9N2O3Cl |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 22978-25-2 |
| PubChem ID | 644213 |
| InChI Key | DNTSIBUQMRRYIU-UHFFFAOYSA-N |
| Smiles | [O-][N+](=O)C1=CC(C(=O)NC2=CC=CC=C2)=C(Cl)C=C1 |
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 | 27.67 | 100 | |
| ethanol | 6.92 | 25mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 276.68. 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 | 3.61 mL | 18.07 mL | 36.14 mL |
| 5 mM | 0.72 mL | 3.61 mL | 7.23 mL |
| 10 mM | 0.36 mL | 1.81 mL | 3.61 mL |
| 50 mM | 0.07 mL | 0.36 mL | 0.72 mL |
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References
References are publications that support the products' biological activity.
Bendixen et al (2001) IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor γ1. Proc.Natl.Acad.Sci.U.S.A. 98 2443 PMID: 11226258
Leesnitzer et al (2002) Functional consequences of cysteine modification in the ligand binding sites of peroxisone proliferator activated receptors by GW9662. Biochemistry 41 6640 PMID: 12022867
Seargent et al (2004) GW9662, a potent antaognist of PPARγ, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARγ agonist rosiglitazone, independently of PPARγ activation. Br.J.Pharmacol. 143 933 PMID: 15533890
Keywords: GW 9662, supplier, Selective, PPARγ, PPARgamma, antagonists, Peroxisome, Proliferator-activating, Receptors, PPAR, GW9662, PPARgamma, Receptors, PPARgamma, Receptors, Tocris Bioscience
