A cell-permeable, selective and irreversible PPARγ antagonist (IC50 = 3.3 nM, 32 nM, and 2 μM for PPARγ, PPARα, and PPARδ, respectively). Reported to covalently modify a cysteine residue in the binding site of PPAR. At a concentration of 10 μM, also acts as an agonist of human pregnane X receptor (PXR) and farnesoid X receptor (FXR). Does not activate liver X receptor-a (LXRa), retinoic acid receptor (RAR), retinoid X receptor-a (RXRa) and thyroid receptors a and b (TRa and TRb) |