Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Bendixenet 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
Leesnitzeret al (2002) Functional consequences of cysteine modification in the ligand binding sites of peroxisone proliferator activated receptors by GW9662. Biochemistry 41 6640 PMID: 12022867
Seargentet 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