Holiday Notification: Cayman Chemical will be closed Monday, May 28, 2012, in observance of the Memorial Day holiday.
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Bezafibrate is a well established pan-peroxisome proliferator-activated receptor (pan-PPAR) activator. This fibrate drug has over 25 years of therapeutic use with a good safety profile. The fibrate class of drugs are generally known as PPARα agonists, but bezafibrate appears to activate PPARδ and PPARγ as well. Bezafibrate activates human PPARα, PPARδ, and PPARγ with EC50 values of 50, 20, and 60 µM, respectively, in a cell-based transcription assay.1 Bezafibrate is used to treat hyperlipidemia. It helps lower low-density lipoprotein cholesterol and triglycerides while raising high-density lipoprotein cholesterol levels. It also improves insulin sensitivity and reduces blood glucose levels, which in combination with the cholesterol effects significantly lowers the incidence of cardiovascular events and development of diabetes in patients with features of metabolic syndrome.2
1
Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J Med Chem43(4)528-550(2000).
2
Tenenbaum, A., Motro, M., and Fisman, E.Z. Dual and pan-peroxisome proliferator-activated receptors (PPAR) co-agonism: The bezafibrate lessons. Cardiovasc Diabetol4(14)1-5(2005).
Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J Med Chem43(4)528-550(2000).
Tenenbaum, A., Motro, M., and Fisman, E.Z. Dual and pan-peroxisome proliferator-activated receptors (PPAR) co-agonism: The bezafibrate lessons. Cardiovasc Diabetol4(14)1-5(2005).
Bezafibrate is available in the following screening
library: