human pparγ

Muraglitazar (BMS-298585) is a dual agonist of PPARα/γ that exerts metabolic regulatory effects including lipid modulation, glucose reduction, improvement of insulin resistance, and weight loss. It is indicated for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar exhibits potent in vitro activity against human PPARα (EC50 = 320 nM) and PPARγ (EC50 = 110 nM).

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

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

Balaglitazone is a selective peroxisome proliferator-activated receptor (PPARγ) partial agonist with an EC50 value of 1.351 μM for human PPARγ.Balaglitazone can be used as a supplement to insulin therapy, regulates blood glucose, and can be used in studies of heart failure and myocardial infarction.

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.

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.

AVE-8134 is an agonist of PPARα. For human and rodent PPARα receptor, the EC50 values are 100 and 3000 nM, respectively.

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).

Pioglitazone (U 72107) is a PPARγ agonist with EC50 of 0.93 and 0.99 μM on human and mouse PPARγ, respectively, and has selective and oral activity. Pioglitazone can be used in diabetes research.

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

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.

Bezafibrate (BM15075) is an antilipemic agent that lowers CHOLESTEROL and TRIGLYCERIDES. It decreases LOW-DENSITY LIPOPROTEINS and increases HIGH-DENSITY LIPOPROTEINS.

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

2,3-Butanediol, derived from the bioconversion of natural resources, holds significant potential for various industries, including chemical, cosmetics, agriculture, and pharmaceutical sectors.

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.

NXT629 is a selective and highly efficient PPAR-α antagonist with anticancer activity. It inhibits PPARδ, PPARγ, Erβ, GR, and TRβ and can be used in research on ovarian cancer and melanoma.

N-Oleoyl Glycine, a Lipoamino Acid, Stimulates Adipogenesis Associated With Activation of CB1 Receptor and Akt Signaling Pathway in 3T3-L1 Adipocyte

Perfluorotetradecanoic acid (PFTeDA) is a PPARγ antagonist. It binds to the ligand-binding domain of human PPARγ, with an IC50 of 22.8 μM and a Kd of 157.8 μM. Perfluorotetradecanoic acid inhibits Leydig cell function by inducing oxidative stress and apoptosis (Apoptosis). Although it stimulates corticosterone biosynthesis, it inhibits aldosterone production.

PPARγ/δ modulator 2 (Compound 3h) functions as a PPARγ agonist and a PPARδ antagonist, with Ki values for PPARγ and PPARδ of 2.8 μM and 43 nM, respectively. It significantly enhances adiponectin production and promotes adipogenic differentiation in human bone marrow-derived mesenchymal stem cells (hBM-MSCs). This compound is applicable in research on metabolic diseases related to hypoadiponectinemia.

12-Nitrolinoleate is a linoleic acid derivative that acts as an agonist of peroxisome proliferator-activated receptor γ (PPARγ). Formed via exposure to acidified nitrite, it is present in human red blood cells and plasma. This compound stimulates PPARγ-dependent gene expression, demonstrated in a reporter assay with MCF-7 cells expressing human PPARγ, with an EC50 of 0.045 µM. At 2.5 µM, 12-Nitrolinoleate reduces the secretion of IL-6, TNF-α, and chemokine (C-C motif) ligand 2 (CCL2) in THP-1 and RAW 264.7 macrophages, and it suppresses LPS-induced NF-κB transcriptional activity in RAW 264.7 macrophages. Additionally, it inhibits TNF-α-induced increases in vascular cell adhesion molecule-1 (VCAM-1) in human umbilical vein endothelial cells (HUVECs) and enhances heme oxygenase-1 (HO-1) levels in primary human aortic endothelial cells at concentrations of 1, 5, or 10 µM.

Prostaglandin A3 is a non-enzymatic dehydration product of prostaglandin E3 (PGE3). It demonstrates significant affinity for canine EP2 and EP4 receptors with IC50 values of 120 nM and 20 nM, respectively. For human PPARγ, Prostaglandin A3 has a Ki value of 188 μM.

EL244 is an inhibitor of Autotaxin (ATX) with an IC50 of 50 nM and an agonist of PPARγ with an IC50 of 1.3 μM and a Kd of 1.3 μM. In human HepG2 cells, EL244 exhibits low cytotoxicity with an EC50 of 81.2 μM and minimal inhibition of cardiac hERG potassium channels (12% at 25 μM). In vivo, EL244 significantly reduces pulmonary lysophosphatidic acid levels, alleviates fibrosis, restores respiratory function, and has limited systemic absorption. EL244 is suitable for research on idiopathic pulmonary fibrosis.

LT175, a dual PPARα/γ ligand, demonstrates potent insulin-sensitizing effects with reduced adipogenic properties. This orally active partial agonist targets PPARγ with EC50 values of 0.22 μm for hPPARα, 0.26 μm for mPPARα, and 0.48 μm for hPPARγ. LT175 specifically interacts with PPARγ, influencing the recruitment of coregulators, such as the cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1), within a hydrophobic region known as the diphenyl pocket [1].

GW 9578 is a selective and potent PPARα agonist with potent lipid-lowering activity for the study of psoriasis, arthritis, alopecia, asthma and type I diabetes.