peroxisome

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 indicated for the treatment of type 2 diabetes, and has been linked to rare instances of acute liver injury.

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.

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.

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

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

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

YM 16638 is an orally active leukotriene (LT) antagonist with triglyceride-lowering and peroxisome-increasing effects that can be used to study antigen-induced early and late airway responses in allergic sheep.

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

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.

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.

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.

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

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.

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).

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.

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.

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

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

GW 501516 (Endurobol) is a effective and highly specifc PPARβ δ agonist (EC50: 1 nM), with 1000-fold selectivity over hPPARα γ.

Pioglitazone hydrochloride (AD 4833) is the hydrochloride salt of an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

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.

Fenofibric acid (FNF acid) is the active form of fenofibrate, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity.

Gliquidone (AR-DF 26) is a potent, second-generation sulfonylurea with antihyperglycemic activity, exhibiting greater binding affinity to SUR1 and increased potency compared to first-generation compounds. Additionally, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.