tcsc1102 GW9662

GW9662 is a potent and selective PPARγ antagonist with an IC₅₀ of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.

IC50 & Target: IC50: 3.3 nM/32 nM/2 μM (PPARγ/α/δ)^[1]

In Vitro: 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^[1]. Co-treatment with both 50 μM Rosiglitazone and 10 μM GW9662 results in statistically lower viable cell numbers after 7 days when compared to treatment with either 50 μM rosiglitazone (P=0.001) or 10 μM GW9662 (P=0.01) alone^[2].

In Vivo: 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^[3]. GW9662 (1 mg/kg, i.p.) largely attenuates the renoprotective effects of Lipopolysaccharide (LPS) in the rat^[4].