PPARγ

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.

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.

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.

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.

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

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.

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.

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.

(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.

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

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.

(S)-(+)-Ibuprofen (Dexibuprofen) , is a non-steroidal anti-inflammatory drug (NSAID), inhibiting cyclooxygenase (COX).

Rosiglitazone maleate (BRL 49653) is the maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

Rosiglitazone hydrochloride (BRL-49653 HCl) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

Magnolol (5,5'-Diallyl-2,2'-biphenyldiol) is a dual agonist of RXRα( EC50=10.4 μM) and PPARγ(EC50=17.7 μM). It blocks TNF-α-induced NF-KB activation.

Chiglitazar is a PPAR α γ δ agonist and insulin sensitizer used in the treatment of type 2 diabetes mellitus to lower blood glucose, regulate blood lipids, and have anti-inflammatory and anti-fibrotic effects.

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

PPARγ agonist16 (Compound 4G) is a PPARγ agonist that competitively binds to the ligand-binding domain (LBD) of PPARγ with an IC50 of 1790 nM. It reduces ear swelling in mouse models and exhibits antihyperglycemic activity in mice with Streptozotocin-induced diabetes.

PPARγ agonist15 (Compound 7c) functions as an agonist of PPARγ, inhibiting the expression of α-amylase (HPA) and α-glucosidase (HLAG) with IC50 values of 28.35 µM and 26.21 µM, respectively. It enhances glucose uptake in L6 myotubes and improves glucose homeostasis, insulin sensitivity, and lipid metabolism in a rat model of Streptozotocin-induced diabetes.

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.

PPARγmodulator-2 (Compound (R)-2n) is a reversible modulator of PPARγ, inhibiting the PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. It helps lower blood glucose levels, improves glucose tolerance and insulin sensitivity, and demonstrates antidiabetic activity in db db mouse models.