PPARγ FP-Based Ligand Screening Assay Kit - Green - 1920 Well

Peroxisome proliferator-activated receptors (PPARs) are ligand activated nuclear receptors. Three PPAR subtypes have been identified: ?, ? (also called ? and NUC1), and ?. PPAR? is the most widely studied PPAR and exists in two protein isoforms (?1 and ?2) due to use of an alternative promoter and alternative splicing. PPAR? is primarily expressed in adipose tissue and to a lesser extent in colon, the immune system, and the retina. PPAR? was first identified as a regulator of adipogenesis, but also plays an important role in cellular differentiation, insulin sensitization, atherosclerosis, and cancer. Ligands for PPAR? include fatty acids, arachidonic acid metabolites such as 15-deoxy-D12,14-PGJ2, as well as the thiazolidinedione class of compounds (TZD) which include pioglitazone and rosiglitazone. TZDs are potent, selective PPAR? agonists that lower the hyperglycemia, hyperinsulinemia, and hypertriglyceridemia found in type 2 diabetic subjects and are presently used as oral antidiabetic drugs. The use of these synthetic ligands has increased the understanding of PPAR?s mechanism of activation and subsequent biological effects. By increasing our understanding of PPAR? additional drug candidates may be identified. Caymans PPAR? FP-Based Ligand Screening Assay Kit - Green provides a convenient fluorescence polarization (FP)-based single step assay for screening PPAR? ligands. In this assay, a ligand of PPAR? was conjugated to fluorescein and is used as the displacement probe. Ligands, agonists, and antagonists of PPAR? will displace the fluorescent probe leading to a decrease in FP. The PPAR? FP-Based Ligand Screening Assay Kit is a robust assay with a Z of 0.81 and has a dynamic range of greater than 120 mP units. The assay has been validated using known agonists/ligands of PPAR? (Arachidonic Acid, Rosiglitazone, Troglitazone, etc.) with IC50 values ranging from nanomolar to millimolar concentrations.Application/High Throughput Screening, Application/Inhibitor Screening Assay, Chemical Class/Assay Kits, Chemical Class/Nuclear Receptors, Research Area/Atherosclerosis, Research Area/Diabetes, Research Area/Drug Discovery, Research Area/Endocrinology, Research Area/Inflammation, Research Area/Metabolic Syndrome, Research Area/MetabolismSynonyms :Peroxisome Proliferator-activated Receptor ? FP-Based Ligand Screening Assay Kit - Green