GW-9662 is a potent, irreversible and selective PPARgamma antagonist, which prevented activation of PPARgamma and inhibited growth of human mammary tumour cell lines. GW-9662 may permit use of anti-ER strategies to inhibit breast cancer in ER- patients.
CAS Number: 22978-25-2
Molecular Weight: 276.68
Chemical Name: 2-Chloro-5-nitro- N -phenylbenzamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
GW-9662 inhibits radioligand binding to PPARγ, PPARα, and PPARδ with pIC50s of 8.48±0.27 (IC50=3.3 nM; n=10), 7.49±0.17 (IC50=32 nM; n=9), and 5.69±0.17 (IC50=2000 nM; n=3), respectively. GW-9662 has nanomolar IC50 versus PPARγ and is 10- and 600-fold less potent in binding experiments using PPARα and PPARδ, respectively. In cell-based reporter assays, GW-9662 is a potent and selective antagonist of full-length PPARγ. Co-treatment with both 50 μM BRL 49653 and 10 μM GW-9662 results in statistically lower viable cell numbers after 7 days when compared to treatment with either 50 μM BRL 49653 (P=0.001) or 10 μM GW-9662 (P=0.01) alone.
Bone marrow (BM) nucleated cell counts in both BADGE- and GW-9662(1 mg/kg, i.p.)-treated mice are significantly higher than counts in the aplastic anemia (AA) group. GW-9662 (1 mg/kg, i.p.) largely attenuates the renoprotective effects of Lipopolysaccharide (LPS) in the rat.
- Jaudszus A, Lorkowski S, Gruen M, Roth A, Jahreis G. Limited Applicability of GW9662 to Elucidate PPARγ-Mediated Fatty Acid Effects in Primary Human T-Helper Cells. Int J Inflam. 2014;2014:149628. doi: 10.1155/2014/149628. Epub 2014 Jun 25. PubMed PMID: 25054074; PubMed Central PMCID: PMC4099290.
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