PPAR 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.

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

MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC₅₀ of 30 nM) and leukotriene biosynthesis (IC₅₀s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.

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.

BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC₅₀ of 0.17 nM.

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

SR 16832 is a dual-site covalent, orthosteric and allosteric PPARγ antagonist. SR 16832 activates the TGF-β signaling pathway and upregulates the expression of Vimentin and Fibronectin (Fibronectin). SR 16832 is toxic to bronchial epithelium. SR 16832 can be used in research related to type 2 diabetes and pulmonary fibrosis.

H-​Trp-​Glu-​OH is a selective, reversible and cell-permeable PPARγ with a K_d of ~8 µM. H-​Trp-​Glu-​OH might be developed as a possible lead compound in diabetes research.

1-O-Hexadecylglycerol can up-regulate PPAR-γ expression, inhibit pGE2, and exhibit anti-inflammatory properties. 1-O-Hexadecylglycerol is effective in oral administration.

SR 11023 is an orally active antagonist of PPARγ, with the IC₅₀ value of 109 nM that plays an important role in diabetic research.

BAY-0069 is a potent and selective PPARγ inverse agonist with an IC₅₀ value of 6.3 nM and 24 nM for human PPARγ and mouse PPARγ. BAY-0069 can be used to research cancer.

MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC₅₀ of 30 nM) and leukotriene biosynthesis (IC₅₀s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis.

GW9662-d₅ is the deuterium labeled GW9662. 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.

Leriglitazone-d₄ (MIN-102-d₄; Hydroxypioglitazone-d₄) is deuterium labeled Leriglitazone. Leriglitazone is an orally active and a BBB-penetrable PPARγ agonist with an EC₅₀ of 9 μM. Leriglitazone, as a regulator of mitochondrial function, has neuroprotective, anti-inflammatory and antioxidant effects. Leriglitazone can be used in the study of neuroinflammatory and neurodegenerative diseases.

Anti-osteoporosis agent-10 is an osteoporosis inhibitor. Anti-osteoporosis agent-10 can suppress the generation of osteoclasts, with an IC₅₀ of 0.042 μM. Anti-osteoporosis agent-10 also has antagonistic activity on PPARγ, with an EC₅₀ value of 0.75 μM.