PPARγ 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.

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.

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

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.

13 (S)-HOTrE is an oxylipin metabolite of α-Linolenic acid (HY-N0728). 13 (S)-HOTrE mediates the inactivation of the NLRP3 inflammasome through the PPAR-γ pathway to exert anti-inflammatory effects. 13 (S)-HOTrE inhibits NF-κB nuclear translocation, ROS production, autophagy and IL-1β levels, induces apoptosis, and increases IL-10 levels. 13 (S)-HOTrE alleviates LPS-induced inflammatory responses in macrophages, prolongs the survival time of septic mice, and regulates the immunometabolic phenotype in parenteral nutrition mouse models. 13 (S)-HOTrE can be used in the research of immune and inflammation-related diseases.

SR-1903 is an inverse agonist of RORγ and PPARγ (IC₅₀ of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models.