货号：G1131

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。 

产品描述

GW9662 is a selective and irreversible PPARγ antagonist with IC50 value of 5.4nM, 10- and 600-fold selectivity against PPARα and PPARδ with IC50 values of 39nM and 1.2μM, respectively. GW9662 had no effect on the ability of any of the PPARs to form heterodimers with RXR. GW9662 could dose-dependently antagonize PPARγ-GAL4-mediated transcription induced by rosiglitazone with IC50 value of 7.6nM. Consistent with this, rosiglitazone-induced increases in aP2 and Oil Red O staining could be completely blocked in C3H10T1/2 cells treated with 1μM GW9662, suggesting the anti-adipogenesis function of GW9662. GW9662 within 2μM clearly blocked the ability of IL-4 (0.1, 0.5ng/ml, but not 1ng/ml) to suppress RANKL/M-CSF-induced osteoclastogenesis in bone marrow monocytes through inhibition of PPARγ1. GW 9662 at concentration of 1μM could antagonize the potentiation of HL-60 cell differentiation induced by PGD2, PGJ2, indomethacin and MPA post 4 days.

作用机制

GW9662 exhibited a competition binding assay against the human ligand binding domain and covalently modified Cys of PPARγ. 

产品信息