Bezafibrate-d4 is intended for use as an internal standard for the quantification of bezafibrate by GC- or LC-MS. Bezafibrate is a non-selective agonist of peroxisome proliferator-activated receptors (PPARs; EC50s = 50, 60, and 20 μM for human PPARα, PPARγ, and PPARδ, respectively).1 It reduces triglyceride levels and the size of lipid droplets in an oleic acid-induced HepaRG hepatocyte model of steatosis when used at a concentration of 25 μM.2 Bezafibrate (10 mg/kg per day) reduces plasma VLDL and LDL mass and triglyceride and free fatty acid levels in a high-fructose plus lard diet-induced rat model of insulin resistance.3
|1. Willson, T.M., Brown, P.J., Sternbach, D.D., et al. The PPARs: From orphan receptors to drug discovery. J. Med. Chem. 43(4), 527-550 (2000).|2. Rogue, A., AnthÉrieu, S., Vluggens, A., et al. PPAR agonists reduce steatosis in oleic acid-overloaded HepaRG cells. Toxicol. Appl. Pharmacol. 276(1), 73-81 (2014).|3. Matsui, H., Okumura, K., Kawakami, K., et al. Improved insulin sensitivity by bezafibrate in rats: Relationship to fatty acid composition of skeletal-muscle triglycerides. Diabetes 46(3), 348-353 (1997).