REVIEW GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM with at least 100 to 1000-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ., respectively. IC50 Value: 3.3 nM(for PPARγ); 32 nM(for PPARα); 2 uM(for PPARδ) Target: PPARγ in vitro: GW9662 is a selective PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively). GW9662 blocks the inhibition of osteoclast formation induced by IL-4 in the low micromolar range (1-2 μM), therefore is more potent than BADGE. PPARγ antagonist GW9662 may inhibit the foam-cell formations in atherosclerosis. GW9662 induces functional estrogen receptor in mouse mammary organ culture. Anticancer, inhibits growth of human mammary tumor cell lines. The induction of ER-α by GW9662, including newer analogs, may permit use of anti-ER strategies to inhibit breast cancer in ER-patients. in vivo: Pretreatment with LPS (1 mg/kg i.p.) significantly attenuates all markers of renal injury and dysfunction caused by ischemia/reperfusion (I/R) injury in rats. Most notably, GW9662 (1 mg/kg i.p.) abolishes the protective effects of LPS.
REFERENCES
[1]
Leesnitzer LM, Parks DJ, Bledsoe RK et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry. 2002 May 28;41(21):6640-50.
[2]
Seargent JM, Yates EA, Gill JH. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec;143(8):933-7. Epub 2004 Nov 8.
[3]
Collino M, Patel NS, Lawrence KM, et al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug;68(2):529-36.
[4]
Karen K Ryan, Bailing Li, Bernadette E Grayson, et al. A role for central nervous system PPAR-γ in the regulation of energy balance. Nature Medicine, 2011,17, 623-626.
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