GSK0660 is a potent, selective, dual PPARβ/δ antagonist with pIC50 of 6.8 (160 nM), shows no activity on PPARα and PPARγ (IC50>10 uM).
GSK0660 antagonizes 100% of the activity of PPARβ/δ with a pIC50 of 6.53, reduces CPT1a expression in skeletal muscle cells with EC50 of 100 nM, as well as ANGPTL4 but not PDK4.
GSK0660 significantly reduces inhibitory effect of GW501516 on the LPS-induced expression of gp91phox mRNA in BV-2 cells.
