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.

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.

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.

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.

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.

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

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.

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.

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.

Oleuropein is an antioxidant polyphenol isolated from olive leaf.

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.

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.

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

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.

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.

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

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

Glabrone shows antiviral activity against influenza virus.

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

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.

Linotroban（CL-871502） is a potent selective thromboxane (TXA2) receptor antagonist with antithrombotic activity.

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

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

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

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.

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

Elafibranor (GFT505) is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

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.

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).

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

Tetramethylkaempferol is a PPARγ agonist, it can improve insulin sensitivity by increasing the levels of adiponectin, an important adipocytokine associated with insulin sensitivity in adipose tissue. Tetramethylkaempferol can concentration-dependently enh

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

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

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).

(±)4-HDHA (4-Hydroxy docosahexaenoic acid) is a PPARγ agonist with anti-inflammatory activity that directly inhibits endothelial cell proliferation and sprouting angiogenesis via PPARγ, which can be used in the study of diabetes.

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.

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.

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.

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).

T0070907(IC50=1 nM) , an effective and specific PPARγ inhibitor, with the >800-fold selectivity over PPARα and PPARδ.

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.

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.

Licochalcone E is a potential LXRβ agonist.

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

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

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

GSK0660 is an antagonist and inverse agonist of PPARβ/δ.