| References |
| Synonyms |
- Peroxisome Proliferator-activated Receptor γ FP-Based Ligand Screening Assay Kit - Green
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| Stability |
6 months |
| Storage |
-20°C |
| Shipping |
Wet ice
in continental US; may vary elsewhere
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Background Reading
Clark, R.B. The role of PPARs in inflammation and immunity. J Leukoc Biol 71 388-400 (2002).
Usui, S., Suzuki, T., Hattori, Y., et al. Design, synthesis, and biological activity of novel PPARγ ligands based on rosiglitazone and 15d-PGJ2. Bioorg Med Chem Lett 15 1547-1551 (2005).
Kersten, S., Desvergne, B., and Wahli, W. Roles of PPARs in health and disease. Nature 405 421-424 (2000).
Sakamoto, J., Kimura, H., Moriyama, S., et al. Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. Biochem Biophys Res Commun 278 704-711 (2000).
Zhang, J., Chung, T.D.Y., and Oldenburg, K.R. A simple statistical parameter for use in evaluation and validation of high throughput screening assays. J Biomol Screen 4(2) 67-73 (1999).
Vidal-Puig, A., Jimenez-Linan, M., Lowell, B.B., et al. Regulation of PPAR γ gene expression by nutrition and obesity in rodents. J Clin Invest 97 2553-2561 (1996).
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| Size |
Global Purchasing |
| 384 wells |
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| 1920 wells |
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Description
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.1 PPARγ is primarily expressed in adipose tissue and to a lesser extent in colon, the immune system, and the retina.2 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.3 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.4,5 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 FP-Based Ligand Screening Assay Kit - Green 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 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 PPARγ (Arachidonic Acid, Rosiglitazone, Troglitazone, etc.) with IC50 values ranging from nanomolar to millimolar concentrations.
1
Vidal-Puig, A., Jimenez-Linan, M., Lowell, B.B., et al. Regulation of PPAR γ gene expression by nutrition and obesity in rodents. J Clin Invest 97 2553-2561 (1996).
2
Clark, R.B. The role of PPARs in inflammation and immunity. J Leukoc Biol 71 388-400 (2002).
3
Usui, S., Suzuki, T., Hattori, Y., et al. Design, synthesis, and biological activity of novel PPARγ ligands based on rosiglitazone and 15d-PGJ2. Bioorg Med Chem Lett 15 1547-1551 (2005).
4
Kersten, S., Desvergne, B., and Wahli, W. Roles of PPARs in health and disease. Nature 405 421-424 (2000).
5
Sakamoto, J., Kimura, H., Moriyama, S., et al. Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. Biochem Biophys Res Commun 278 704-711 (2000).
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