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.
Chemical Formula: C13H9ClN2O3
Exact Mass: 276.03017
Molecular Weight: 276.67
Elemental Analysis: C, 56.43; H, 3.28; Cl, 12.81; N, 10.13; O, 17.35
2-Chloro-5-nitro- N -phenylbenzamide
InChi Code: InChI=1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17)
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
GW9662 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. GW9662 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, GW9662 is a potent and selective antagonist of full-length PPARγ. Co-treatment with both 50 μM BRL 49653 and 10 μM GW9662 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 GW9662 (P=0.01) alone.
Bone marrow (BM) nucleated cell counts in both BADGE- and GW9662(1 mg/kg, i.p.)-treated mice are significantly higher than counts in the aplastic anemia (AA) group. GW9662 (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.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.