PPARβ/δ Antagonist

GW9662 is a potent and selective PPARγ antagonist with an IC₅₀ of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.

T0070907 is a potent PPARγ antagonist with a K_i of 1 nM.

GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC₅₀ of 6.6.

GSK0660 is a potent PPARβ antagonist with an IC₅₀ of 155 nM.

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. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.

DG172 dihydrochloride is a selective PPARβ/δ antagonist, with an IC₅₀ of 27 nM.

F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC₅₀ value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.

PT-S58, a GSK0660 derivative, is a PPARβ/δ full antagonist with an IC₅₀ value of 98 nM. PT-S58 inhibits the agonist-induced transcriptional activity of PPARβ/δ in vitro.

CC618 is a selective PPARβ/δ antagonist. CC618 covalently modifies conserved Cys249 in the PPARβ/δ ligand-binding pocket via nucleophilic aromatic substitution, converting its thiol moiety to a 5-trifluoromethyl-2-pyridylthioether.