PPAR

Ragaglitazar(NNC-61-0029) is a potent dual PPARα and PPARγ agonist that has shown potent lipid-lowering and insulin sensitizing effects in animal models.Ragaglitazar can be used to study type 2 diabetes.

Abietic Acid (Sylvic acid) is the primary component of resin acid isolated from rosin.

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.

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.

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.

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.

2,3-Butanediol is a biotransformed butanediol derived from natural resources.

PHYTOL (trans-Phytol) , a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.

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

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

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

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.

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

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

MK-0533 is a novel PPARγ partial agonist for the prevention of vascular endothelial dysfunction (VED) and VED-related cardiovascular disease.

Cevoglitazar (LBM-642) is a PPARɑ agonist and PPARγ agonist. Cevoglitazar potently reduces food intake and body weight in obese mice and cynomolgus monkeys.

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

Sulotroban potassium is a small molecule thromboxane A2 receptor (TXA2R) antagonist that can be used to study myocardial infarction and thrombosis.

Dazmegrel (UK 38,485) is a potent and specific thromboxane A2 (TXA2) synthase inhibitor for the prevention of increased whole platelet aggregation in normal pregnancy.

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

FUREGRELATE, a thromboxane A2 (TxA2) synthase inhibitor, blunts the development of pulmonary arterial hypertension in neonatal piglets.

KD-3010 (Kalypsys) is an orally active potent and selective PPARδ agonist for the study of liver injury.

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

CGS 15435 is a potent thromboxen (TxA2) synthetase inhibitor (IC50: 1 nM). CGS 15435 acts on PGI2 synthase, cyclooxygenase and liposynthase with much less selectivity than on thromboxin synthase.

CC618 is a selective PPARβ/δ antagonist with an IC50 of 10.0 μM.

Imiglitazar (TAK559) is a potent PPAR-β δ receptor agonist with hypoglycemic effects.

Lonazolac is a nonsteroidal anti-inflammatory drug[1].

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.

WAY-620472 is a PPAR regulator that can be used to alter the lifespan of eukaryotes.

Benzo[b]thiophene-7-propanoic acid, α-methoxy-4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-, (αR)- is a dual PPARα/γ agonist with EC50 of 0.358μM and 1.21μM. Benzo[b]thiophene-7-propanoic acid, α-methoxy-4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-, (αR)- is the R-isomer of Aleglitazar.

G3335 Acetate was discovered to be a novel PPARgamma antagonist.

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.

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

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.

Inolitazone dihydrochloride is an effective, high-affinity PPARγ agonist; its biological activity is dependent on PPARγ (IC50:0.8 nM) to inhibit cell growth. Inolitazone dihydrochloride enhances the role of cell cycle kinase inhibitor p21 WAF1/CIP1.

Furegrelate sodium (U-63557A) is a selective thromboxane synthase inhibitor with oral activity. Furegrelate sodium(U-63557A) inhibits thromboxane A2 (TXA2) synthase in human platelet microsomes with an IC50 of 15 nM.

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

MSDC-0602K (Azemiglitazone potassium) (Azemiglitazone potassium) is a PPARγ-sparing thiazolidinedione (Ps-TZD) compound that binds to PPARγ with an IC50 of 18.25 μM. It also modulates the mitochondrial pyruvate carrier (MPC). This compound, MSDC-0602K, has potential applications in researching fatty liver conditions, including dysfunctional lipid metabolism, inflammation, and insulin resistance. MSDC-0602K acts as an insulin sensitizer, improving insulinemia and fatty liver disease in mice both individually and in combination with Liraglutide.

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.

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

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.

Daltroban (SKF 96148) is a specific thromboxane A2 (TXA2) receptor antagonist. Daltroban shows protective effect in reperfusion injury. Daltroban increase intracellular calcium in vascular smooth muscle cells.

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.

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).

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

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.

Alliin ((S)-3-(Allylsulphinyl)-L-alanine) is a garlic organosulfur compound that possesses various pharmacological properties.alliin protected against LPS-induced ALI by activating PPARγ, which subsequently inhibited LPS-induced NF-κB activation and inflammatory response. Alliin might be used as an anti-inflammatory agent in the treatment of ALI.