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.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|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|
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
If you know of a relevant reference for GW 9662, please let us know.
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Keywords: GW 9662, supplier, Selective, PPARγ, PPARgamma, antagonists, Peroxisome, Proliferator-activating, Receptors, PPAR, GW9662, PPARgamma, Receptors, PPARgamma, Receptors, Tocris Bioscience
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
Do you know of a great paper that uses GW 9662 from Tocris? If so please let us know.
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