Metabolism

GW6471 is a PPARα antagonist, shown to completely inhibit GW409544-induced activation of PPARα.

GSK-2033 is a potent cell-active LXR antagonist (pIC50 = 7.5). It enhances T-cell proliferation and blocks T 0901317-antiproliferative activity on T-cells and is cell permeable.

NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively.

GW 6471 is a potent PPARα antagonist.

BAY 2416964 is a potent and orally active aryl hydrocarbon receptor (AHR) antagonist extracted from patent WO2018146010A1, example 192, has an IC50 of 341 nM. BAY 2416964 has the potential for solid tumors treatment.