||GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ.
||Elafibranor, also known as GFT-505, is a dual PPARα/δ agonist. Elafibranoris currently being studied for the treatment of cardiometabolic diseases including diabetes, insulin resistance, dyslipidemia, and non-alcoholic fatty liver disease (NAFLD).
||Bavachinina is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50?=?0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively).
||Troglitazone, also known as CI991, is a potent PPAR agonist. Troglitazone is an antidiabetic and anti-inflammatory drug, and a member of the drug class of the thiazolidinediones. It was prescribed for patients with diabetes mellitus type 2 in Japan Troglitazone, like the other thiazolidinediones (pioglitazone and rosiglitazone), works by activating peroxisome proliferator-activated receptors (PPARs). Troglitazone is a ligand to both PPARα and – more strongly – PPARγ
||Glabridin, one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
||Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist.
||Bezafibrate is an agonist of peroxisome proliferator-activated receptor alpha (PPARalpha) with antilipidemic activity. Bezafibrate is a fibrate drug used for the treatment of hyperlipidaemia. Bezafibrate decreases triglyceride levels, increases high density lipoprotein cholesterol levels, and decreases total and low density lipoprotein cholesterol levels. It is commonly marketed as Bezalip
||GW0742, also known as GW610742 and GW0742X is a PPARδ/β agonist. GW0742 Induces Early Neuronal Maturation of Cortical Post-Mitotic Neurons. GW0742 prevents hypertension, vascular inflammatory and oxidative status, and endothelial dysfunction in diet-induced obesity. GW0742 has direct protective effects on right heart hypertrophy.GW0742 may enhance lipid metabolism in heart both in vivo and in vitro.
||Pioglitazone Hydrochloride is a thiazolidinedione compound described to produce antiinflammatory and antiarteriosclerotic effects. Pioglitazone is demonstrated to prevent L-NAME-induced coronary inflammation and arteriosclerosis and to suppress increased TNF-α mRNA produced by aspirin-induced gastric mucosal injury. Pioglitazone Hydrochloride is an activator of PPAR γ
||Rosiglitazone is an antidiabetic drug in the thiazolidinedione class of drugs. It works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin. Rosiglitazone is a member of the thiazolidinedione class of drugs. Thiazolidinediones act as insulin sensitizers. They reduce glucose, fatty acid, and insulin blood concentrations. They work by binding to the peroxisome proliferator-activated receptors (PPARs). PPARs are transcription factors that reside in the nucleus and become activated by ligands such as thiazolidinediones. Thiazolidinediones enter the cell, bind to the nuclear receptors, and alter the expression of genes.
||GSK0660 is a selective PPARδ antagonist. GSK0660 differentially regulated 273 transcripts in TNFα-treated cells compared to TNFα alone. A pathway analysis revealed the enrichment of cytokine-cytokine receptor signaling. In particular, GSK0660 blocks the TNFα-induced upregulation of CCL8, a chemokine involved in leukocyte recruitment. GSK0660 blocks the effect of TNFα on the expressions of cytokines involved in leukocyte recruitment, including CCL8, CCL17, and CXCL10 and it may therefore block TNFα-induced retinal leukostasis.
||Oroxin A, an active component isolated from the herb Oroxylum indicum (L.) Kurz, activates PPARγ and inhibits α-glucosidase, exerting antioxidant activity.
||AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows 5 nM Wnt pathway inhibition in DLD-1 cells. AZ6102 can be formulated well in a clinically relevant intravenous solution at 20 mg/mL, has demonstrated good pharmacokinetics in preclinical species, and shows low Caco2 efflux to avoid possible tumor resistance mechanisms. The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis, and cancer. Germline mutations of several Wnt pathway components, such as Axin, APC, and ?-catenin, can lead to oncogenesis. Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is known to inhibit the Wnt pathway via increased stabilization of Axin.
||KRP297, also known as MK-0767 and MK-767, is a PPAR agonist potentially for the treatment of type 2 diabetes and dyslipidemia. When administered to ob/ob mice, KRP-297 (0.3 to 10 mg/kg) decreased plasma glucose and insulin levels and improved the impaired insulin-stimulated 2DG uptake in soleus muscle in a dose-dependent manner. KRP-297 treatment is useful to prevent the development of diabetic syndromes in addition to ameliorating the impaired glucose transport in skeletal muscle.
||Inolitazone, also known as Efatutazone, CS-7017, and RS5444, is an orally bioavailable PAPR-gamma inhibitor with potential antineoplastic activity. Inolitazone binds to and activates peroxisome proliferation-activated receptor gamma (PPAR-gamma), which may result in the induction of tumor cell differentiation and apoptosis, as well as a reduction in tumor cell proliferation. PPAR-gamma is a nuclear hormone receptor and ligand-activated transcription factor controlling gene expression involved in such cellular processes as differentiation, apoptosis, cell-cycle control, carcinogenesis, and inflammation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
||GW6471 is a PPAR α antagonist (IC50 = 0.24 μ M). GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.
||Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist.