GW 9662

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Cat.No. 1508 - GW 9662 | C13H9N2O3Cl | CAS No. 22978-25-2
Description: Selective PPARγ antagonist
Chemical Name: 2-Chloro-5-nitro-N-phenylbenzamide
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Literature

Biological Activity

Selective 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.

Select a batch to recalculate based on the batch molecular weight:
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
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Safety Datasheet

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


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Keywords: Selective PPARγ PPARgamma antagonists Peroxisome Proliferator-activating Receptors PPAR GW9662 PPARgamma Receptors

6 Citations for GW 9662

Citations are publications that use Tocris products. Selected citations for GW 9662 include:

Ramachandran et al (2012) Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer. J Biol Chem 287 38028 PMID: 22992727

Mottillo et al (2012) Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. PLoS One 287 25038 PMID: 22685301

Scuderi et al (2012) Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α. Arterioscler Thromb Vasc Biol 9 49 PMID: 22405189

Esposito et al (2011) Cannabidiol reduces Aβ-induced neuroinflammation and promotes hippocampal neurogenesis through PPARγ involvement. FASEB J 6 e28668 PMID: 22163051

Ali et al (2009) Antiplatelet actions of statins and fibrates are mediated by PPARs. J Neurosci 29 706 PMID: 19150877

Ali et al (2006) Role of nuclear receptor signaling in platelets: antithrombotic effects of PPARβ. J Neuroinflammation 20 326 PMID: 16368717


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Literature in this Area

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Pathways for GW 9662

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