PPARα 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.

GW6471 is a selective peroxisome proliferator-activated receptor α (PPARα) antagonist. GW6471 reduces cancer stem cell viability, proliferation, and spheroid formation. GW6471 induces apoptosis and causes metabolic impairment including energy imbalance. GW6471 can be used for the research of paragangliomas and triple-negative breast cancer.

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

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.

Amezalpat is the antagonist for PPARα with IC₅₀ of 58 nM. Amezalpat exhibits antineoplastic activity.

PPARα/δ antagonist-1 is an orally active, highly selective dual antagonist of PPARα/δ, with IC₅₀ values of 0.113 μM and 0.025 μM against human PPARα and PPARδ, respectively. PPARα/δ antagonist-1 exhibits an excellent in vitro activity profile and preliminary efficacy in mouse tumor models. PPARα/δ antagonist-1 can be used in studies related to cancers (melanoma metastasis, ovarian cancer).