BAY-0069 (BAY0069) is a potent, selective, covalent PPARγ inverse agonist with IC50 of 0.22 nM in cellular reporter assays.
BAY-0069 displays no signigicant acitivity against PPARA, PPARD and additional high homology PXR (IC50 values >40 uM).
BAY-0069 inhibits proliferation of PPARG-amplified cell line UM-UC-9 with IC50 of 2.5 nM.
In UM-UC-9 xenograft-bearing mice, BAY-0069 demonstrated a modest downregulation of FABP4 expression, comparable with that of SR10221, despite more robust in vitro inverse agonism in NCOR2 recruitment, RT112-FABP4-NLucP luciferase repression, and UM-UC-9 proliferation.
