GW 9662

GW 9662 is a selective, irreversible, and effective peroxisome proliferator activated receptor-γ (PPARγ) antagonist. PPARγ research demonstrates that GW 9662 covalently modifies Cys(285) and does not affect transcription of full-length PPARα and PPARδ. GW 9662 has been shown to block Rosiglitazone (sc-202795)-mediated activation of PPARγ, and improve growth inhibition induced by Rosiglitazone in breast tumor cell research. Additionally, reports indicate that GW 9662 blocks the protective activity of lipopolysaccharide, LPS, and acts as an agonist for the farnesoid X receptor (FXR) and pregnane X receptor (PXR) nuclear receptors. 参考文献 1. Huang, J.T., et al. 1999. Nature. 400: 378-382. PMID: 10432118 2. Leesnitzer, L.M., et al. 2002. Biochemistry. 41: 6640-6650. PMID: 12022867 3. Seargent, J.M., et al. 2004. Br. J. Pharmacol. 143: 933-937. PMID: 15533890 4. Collino, M., et al. 2005. Kidney Int. 68: 529-536. PMID: 16014029 5. Collin, M., et al. 2006. Crit. Care Med. 34: 1131-1138. PMID: 16484917 6. Davies, G.F., et al. 2009. Drug Des Devel Ther. 3: 79-88. PMID: 19920924

276.7

GW 9662 is a selective, irreversible, and effective PPARγ antagonist that also acts as a FXR and PXR agonist

2-chloro-5-nitrobenzanilide; 2-Chloro-5-nitro-N-phenylbenzamide

C1=CC=C(C=C1)NC(=O)C2=C(C=CC(=C2)[N+](=O)[O-])Cl

C13H9ClN2O3

22978-25-2