PPARγ Ligand Screening Assay Kit – 384 wells

Peroxisome proliferator-activated receptors (PPARs) are ligand activated nuclear receptors. Three PPAR subtypes have been identified: α, β (also called δ and NUC1), and γ. PPARγ is the most widely studied PPAR and exists in two protein isoforms (γ1 and γ2) due to use of an alternative promoter and alternative splicing.{12922} PPARγ is primarily expressed in adipose tissue and to a lesser extent in colon, the immune system, and the retina.{12196} PPARγ was first identified as a regulator of adipogenesis, but also plays an important role in cellular differentiation, insulin sensitization, atherosclerosis, and cancer. Ligands for PPARγ 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.{12961} TZDs are potent, selective PPARγ agonists that lower the hyperglycemia, hyperinsulinemia, and hypertriglyceridemia found in type 2 diabetic subjects and are presently used as oral antidiabetic drugs.{7654,10857} The use of these synthetic ligands has increased the understanding of PPARγ’s mechanism of activation and subsequent biological effects. By increasing our understanding of PPARγ additional drug candidates may be identified. Cayman’s PPARγ Ligand Screening Assay Kit provides a convenient fluorescence polarization (FP)-based single step assay for screening PPARγ ligands. In this assay, a ligand of PPARγ was conjugated to fluorescein and is used as the displacement probe. Ligands, agonists, and antagonists of PPARγ will displace the fluorescent probe leading to a decrease in FP. The PPARγ 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 PPARγ (Arachidonic Acid, Rosiglitazone, Troglitazone, etc.) with IC50 values ranging from nanomolar to millimolar concentrations.