PPAR

Muraglitazar (BMS-298585) is a PPAR α γ dual agonist for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar shows potent activity in vitro at human PPARα and PPARγ with EC50 of 320 nM and 110 nM respectively.

Abietic Acid (Sylvic acid) is a diterpene extracted from Pimenta racemosavar. grissea with antimicrobial, antiproliferative and anti-obesity activities. It inhibits lipoxygenase activity and may be studied in allergic diseases.

GW 7647 is an effective and highly selective PPARα agonist, the EC 50 values of human PPARα, PPARγ and PPARδ receptors are 6,1100 and 6200 nM, respectively. GW 7647 can reduce the production of nitric oxide in macrophages and has lipid-lowering and anti-inflammatory properties in the body.

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.

Farglitazar (GI-262570) is a PPAR-γ agonist and insulin sensitizer that inhibits stellate cell activation by activating receptor γ via oxidative enzymes proliferators and is used in the study of diabetes.

Fucosterol is isolated from E. stolonifera with anti-diabetic, anti-adipogenic and anti-cancer activities. It regulates adipogenesis via modulation of PPARα and C EBPα expression.

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.

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.

Troglitazone (Romglizone) is a PPARγ agonist with anti-inflammatory and anti-tumor activity.

Reglitazar (JTT-501) is a dual PPARα and PPARγ agonist that is used to study diabetes.

Oleuropein is an antioxidant polyphenol isolated from olive leaf.

Astaxanthin (trans-Astaxanthin) is a keto-carotenoid in the terpenes class of chemical compounds. It is classified as a xanthophyll but it is a carotenoid with no vitamin A activity. It is present in most red-colored aquatic organisms. Astaxanthin has shown to mediate anti-oxidant and anti-inflammatory actions. It may be found in fish feed or some animal food as a color additive.

ARH-049020 (ARH049020) is a PPAR agonist used in the study of type 2 diabetes.

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

Saroglitazar (Lipaglyn) is an agonist of PPAR with EC50 values of 0.65 pM and 3 nM for PPARα and PPARγ.

Aleglitazar (R1439) (R1439) is a potent dual PPARα γ agonist, with IC50s of 38 nM and 19 nM for human PPARa and PPARγ, respectively. Aleglitazar can be used for the research of type II diabetes.

Pemafibrate ((R)-K-13675) is a highly specific PPARα agonist (EC50: 1 nM).

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

THR-0921 (CLX-0921) is a peroxisome proliferator-activated receptor (PPAR) agonist that can be used to study cardiovascular and metabolic diseases.

K-111 (BM-170744) is an orally available peroxisome proliferator-activated receptor (PPAR)-alpha agonist and insulin enhancer for the study of obesity-type diabetes mellitus and the metabolic syndrome.

Mavodelpar free acid hydrochloride (Pparδ agonist HCl) is a potent PPARδ agonist.

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.

Suksdorfin has hypoglycemic effects, promotes adipocyte differentiation and enhances lipocalin production, activates peroxisome proliferator-activated receptor gamma (PPARγ), promotes insulin-dependent glucose uptake by adipocytes, and can be used to study obesity.

Glabrone shows antiviral activity against influenza virus.

Icariin (Ieariline) belongs to the flavonol glycoside group of natural products, can inhibit PDE5 and PDE4 activity (IC50=432 73.50 μM), is also a PPARα activator. Icariin can increase cardiovascular and cerebrovascular blood flow, promote hematopoiesis, immunity and bone metabolism.

GW1929 is a potent PPAR-γ agonist (pKi: 8.84 for human PPAR-γ; pEC50s of 8.56 and 8.27 for human and murine PPAR-γ).

Oleoylethanolamide (N-Oleoylethanolamide) is a high affinity endogenous agonist of PPAR-α.

(S)-Coriolic acid (13(S)-HODE) is an important intracellular signaling agent generated by the reaction of linoleic acid with plant and mammalian lipoxygenases. It is involved in cell proliferation and differentiation in various biological systems and inhibits the adhesion of tumor cells to the vascular endothelium, while down-regulating IRGpIIb IIIa receptor expression at around 1 μM. Additionally, (S)-Coriolic acid is a metabolite of 15-lipoxygenase (15-LOX) and often acts as an endogenous ligand to activate PPARγ. It induces mitochondrial dysfunction and airway epithelial damage.

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.

LY518674 (LY-674) decreases triglycerides and increases HDL-C and is used for the treatment of atherosclerosis. LY518674 is an effective and selective PPARα agonist (EC50: 42 nM for human PPARα).

Dihydrocurcumin is the main metabolite of curcumin, which can reduce fat accumulation and oxidative stress response. Dihydrocurcumin can regulate the mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increase the protein expression levels of pAKT and PI3K, and reduce the intracellular NO and ROS contents through Nrf2 signaling pathway.

CDDO-Im (TP-235) is an activator of Nrf2 and PPAR (Kis: 232 344 nM for PPARα PPARγ).

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

GSK376501A is a selective and effective modulator of peroxisome proliferator-activated receptor γ (PPARγ) for the study of type 2 diabetes.

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.

Ciglitazone (ADD 3878) is a potent and selective PPARγ agonist (EC50: 3 μM) and oral hypoglycemic agent. Ciglitazone inhibits proliferation and differentiation of th17 cells, decreases insulin levels, vascular endothelial growth factor production and blood pressure, and induces cell cycle arrest in gastric cancer cells. Selegiline induces apoptosis in opossum kidney epithelial cells and activates nuclear translocation of p38 MAPK and apoptosis-inducing factor (AIF). Ciglitazone exhibits hypoglycaemic activity in animal models of obesity and hyperglycaemia.

Tesaglitazar is a potent and selective peroxide PPARα γ receptor dual agonist with a more potent affinity for PPARγ than PPARα, The EC50 values for rat PPARα and human PPARα were 13.4 μM and 3.6 μM, respectively, and 0.2 μM for rat PPARγ and human PPARγ. Tesaglitazar induced DNA synthesis and fibrosarcoma formation in rat subcutaneous mesenchymal cells.

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.

Ragaglitazar(NNC-61-0029) is a potent dual activator of PPARγ and PPARα, which shows improved insulin sensitization and lipid-lowering potential in animal models and can be used to study type 2 diabetes.

Naringenin (NSC-11855) is a flavanone that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, antiinflammatory, carbohydrate metabolism promoter, immunity system modulater. This substance has also been shown to repair DNA.

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.

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).

Moringin is an isothiocyanate obtained from myrosinase-mediated hydrolysis of the glucosinolate precursor glucoMoringin present in Moringa oleifera seeds. Moringin has anti-inflammatory and antioxidative properties.

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

Palmitoylethanolamide (Impulsin) is an endogenously fatty acid amide. It has a role as an anti-inflammatory drug, an antihypertensive agent, a neuroprotective agent and an anticonvulsant.Upon administration, palmitoylethanolamide may inhibit the release of pro-inflammatory mediators from activated mast cells.

Fisetin belongs to a group of natural flavonols with a variety of biological activities, including anti-inflammatory, antioxidant, anti-tumor, anti-aging and neuroprotective effects.

Licochalcone E is a potential LXRβ agonist.

Sakuranetin, a flavanone phytoalexin from ultraviolet-irradiated rice leaves, it has antifungal, antimutagenic, anti-inflammatory and antioxidant effects