Lanifibranor (IVA337) is an agonist of peroxisome proliferator-activated receptors (PPARs) with EC50 values of 1,537, 866, and 206 nM for human recombinant PPARα, PPARβ, and PPARγ, respectively, for transactivation activity

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

Daidzein (Isoflavone) is an isoflavone extract from soy, which is an inactive analog of the tyrosine kinase inhibitor genistein. It has antioxidant and phytoestrogenic properties.

5-Aminosalicylic Acid (5-ASA) is an anti-inflammatory agent, structurally related to the SALICYLATES, which is active in INFLAMMATORY BOWEL DISEASE. It is considered to be the active moiety of SULPHASALAZINE.

Cinnamyl alcohol (Styryl Carbinol) readily autoxidizes upon air exposure, and forms strong sensitizers as determined by the local lymph node assay.

Icariin (Ieariline) is a flavonol glycoside, inhibiting PDE5 and PDE4 activities. Icariin also is a PPARα activator.

Fenofibrate (Lipanthyl) is a peroxisome proliferator receptor alpha agonist. Fenofibrate is a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.

1. Raspberry ketone (p-Hydroxybenzyl acetone) is cytotoxic to melanocytes through the binding of RK-derived quinones to thiol proteins and the pro-oxidant activity of the RK-oligomer, the exposure of human skin to RK can cause chemical/occupational leukoderma. 2. Raspberry ketone is marketed on the Internet as a food supplement.

LJ570 is the first PPARα/γ dual agonist (PPARα,PPARγ with EC50s of 1.05 and 0.12 μM, respectively[)

Inolitazone (RS5444) a high-affinity PPARγ agonist. Inolitazone exhibits IC50 for growth inhibition is ~0.8 nM in vitro.

Darglitazone (CP-86325) is a potent, selective agonist of PPAR-γ with antidiabetic actions. Darglitazone is effective in controlling blood glucose and lipid metabolism.

MCC-555 (Isaglitazone) is a PPARα and PPARγ agonist exerting antihyperglycemic effects.

SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

Pioglitazone (U 72107) is an insulin sensitizing agent and thiazolidinedione that is indicated for the treatment of type 2 diabetes. Pioglitazone has been linked to rare instances of acute liver injury.

GW9662 (TIMTEC-BB SBB006523) is a specific PPARγ antagonist (IC50: 3.3 nM, in a cell-free assay), with 100 to 1000-fold functional selectivity for PPARγ than PPARα/δ in cells.

Retinoic acid (Tretinoin), a metabolite of vitamin A, is a natural agonist of the retinoic acid receptor RAR and inhibits RARα/β/γ (IC50=14 nM). Retinoic acid induces cellular differentiation, reduces cellular proliferation, and inhibits tumorigenesis.

Fisetin is a natural flavonol extracted from Rhus succedanea L that is structurally and functionally related to kaempferol, can modulate sirtuins,with antioxidant, anticancer, neuroprotection effects.

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, inhibiting 5-lipoxygenase-activating protein (FLAP). It is also a moderately potent PPARα antagonist.

MA-0204 is a highly selective and orally available peroxisome proliferator-activated receptor δ (PPARδ) modulator (EC50s: 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively). It is a potential treatment for Duchene Muscular Dystrophy (DMD).

GQ-16 is a partial agonist of PPARγ with a Ki of 160 nM. GQ-16 reduces adipogenic actions and promotes insulin Sensitization without weight gain.

Bocidelpar is a modulator of PPARδ with an EC50 of 7.80 nM and improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy muscle cells.

NPC 15199 (FMOC-L-Leucine) is an anti-inflammatory agent.

SR 16832 is a dual-site PPARγ inhibitor. It also inhibits the binding of endogenous ligands and transcriptional activity of PPARγ, more effectively than the orthosteric covalent antagonist GW 9662 and T 0070907.

EHP-101 (VCE-004.8) is a specific dual agonist of PPARγ and CB2 receptor with potent anti-inflammatory activity. EHP-101 attenuates adipogenesis and prevents diet-induced obesity.

Highly selective orally active peroxisome proliferator-activated receptor (PPAR)γ agonist (pEC50 values are 8.05, < 4 and < 4 for human PPARγ, PPARα and PPARδ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo. Brown et al (1999) A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-γ reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes 48 1415 PMID:10389847 |Nugent et al (2001) Potentiation of glucose uptake in 3T3-L1 adipocytes by PPARγ agonists is maintained in cells expressing a PPARγ dominant-negative mutant: evidence for selectivity in the downstream responses to PPARγ activation. Mol.Endocrinol. 15 1729 PMID:11579205 |Way et al (2001) Adipose tissue resistin expression is severely suppressed in obesity and stimulated by peroxisome proliferator-activated receptor γ agonists. J.Biol.Chem. 276 25651 PMID:11373275

Oroxin A (Baicalein 7-O-glucoside) has antitussive and expectorant effects.

ZINC08438472 is a selective peroxisome proliferator-activated receptors-α agonist.

Choline Fenofibrate (Trilipix) is a choline formulation of fenofibrate, a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.

Clofibrate (Clofibrato) is an aryloxyisobutyric acid derivate with antihyperlipidemic activity.

Rosiglitazone maleate (BRL 49653) is the maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

Eupatilin (NSC-122413), a flavone derived from Artemisia princepsPampanini, is a PPARα agonist, with pharmacological activity.

Angeloylgomisin H shows moderate cytotoxic activities with IC50 values ranging from 100 to 200 ug/mL against MCF7, HEK293 and CAL27 cell lines.

GW0742 (GW610742) is an effective and specific PPARδ agonist (EC50: 1 nM/1.1 μM/2 μM, for human PPARδ/α/γ).

1. Agrimol B is a main active ingredient isolated from Agrimonia pilosa Ledeb.

Seladelpar (MBX 8025) has been used in trials studying the treatment of Hyperlipidemia.

Pirinixic Acid (NSC 310038) is a synthetic thiacetic acid derivative used in biomedical research, carcinogenic Pirinixic acid is a peroxisome proliferator that activates specific peroxisome proliferator-activated receptors (PPAR).

Arhalofenate (JNJ 39659100) is a selective partial agonist of peroxisome proliferator-activated receptor PPARγ. It is used for the treatment of type 2 diabetes.

AMG131 (CHS 131) , is a novel, non-thiazolidinedione (TZD), selective peroxisome proliferator-activated receptor (PPAR)gamma modulator, which can be used for the treatment of type 2 diabetes mellitus (non-insulin dependent diabetes)

Tetradecylthioacetic acid is a synthetic fatty acid with a sulfur substitution in the β-position. This modification renders TTA unable to undergo complete β-oxidation and increases its biological activity, including activation of peroxisome proliferator activated receptors (PPARs) with preference for PPARα.

Glabridin (KB-289522) may serve as an anti-inflammatory agent in diabetes-related vascular dysfunction, through regulating the synthesis and activity of iNOS under high-glucose levels; may possess a therapeutic effect on metabolic disorders( such as diabetes and hyperglycemia), by modulating glucose metabolism through AMPK in skeletal muscle cells. Glabridin may have potential as a chemopreventive agent against liver Y metastasis, by inhibiting the invasion of human HCC cells.

Ginsenoside Rh1 (Sanchinoside B2) , one of the main constituents of Panax ginseng, exhibits anti-inflammatory effect.

Palmitelaidic Acid (trans-Palmitoleic acid) is one of the most abundant fatty acids in serum and tissue.

Ciprofibrate (Win35833) is a fibrate derivative with antilipidemic activity.

Cloxiquine (Dermofongin) is a monohalogenated 8-hydroxyquinoline with activity against bacteria, fungi, and protozoa.

beta-Amyrone (β-Amyron) has antifungal activity against Chikungunya virus replication with an EC50 of 86 uM. beta-Amyrone has anti-inflammatory activity through inhibiting the expression of COX-2. beta-Amyrone exhibits anti-α-glucosidase inhibitory activity and moderate AChE activity. β-Amyrone can be used in the research of disease like inflammation, infection, and obesity.

Bilobetin ameliorates insulin resistance by PKA-mediated phosphorylation of PPARα in rats fed a high-fat diet.

GW6471 is an antagonist of PPARα with IC50 of 0.24 μ M. GW6471 enhances the binding affinity of the PPAR α ligand-binding domain to the co-repressor proteins SMRT and NCoR.

Norathyriol is a potent PTP1B inhibitor with good cell permeability and oral availability.

1.(-)-Licarin B (Licarine B) has anti-mycobacterial activity.