Fenofibrate-d6

Fenofibrate-d₆ is intended for use as an internal standard for the quantification of fenofibrate by GC- or LC-MS. Fenofibrate is an agonist of peroxisome proliferator-activated receptor α (PPARα) with EC₅₀ values of 18 and 30 μM for mouse and human receptors, respectively, in a transactivation assay.¹ It is selective for PPARα over PPARγ (EC₅₀s = 300 and 200 μM for mouse and human receptors, respectively) and lacks activity at mouse and human PPARδ at a concentration of 100 μM. In vivo, fenofibrate (50-100 mg/kg) reduces plasma levels of triglycerides, C-reactive protein, and malondialdehyde (MDA) in mice with fructose-induced hypertriglycemia in a dose-dependent manner.² It decreases glomerular and tubular atrophy and necrosis induced by cisplatin in rat kidney when administered at a dose of 100 mg/kg.³ Fenofibrate also reduces the number of pulmonary lesions induced by 4-nitroquinoline 1-oxide (4-NQO) in lung of Tsumura Suzuki obese diabetic (TSOD) mice.⁴

1.Willson, T.M., Brown, P.J., Sternbach, D.D., et al.The PPARs: From orphan receptors to drug discoveryJ. Med. Chem.43(4)527-550(2000) 2.Sun, B., Xie, Y., Jiang, J., et al.Pleiotropic effects of fenofibrate therapy on rats with hypertriglycemiaLipids Health Dis.14:27(2015) 3.Helmy, M.M., Helmy, M.W., and El-Mas, M.M.Additive renoprotection by pioglitazone and fenofibrate against inflammatory, oxidative and apoptotic manifestations of cisplatin nephrotoxicity: Modulation by PPARsPLoS One10(11)e0142303(2015) 4.Kuno, T., Hata, K., Takamatsu, M., et al.The peroxisome proliferator-activated receptor (PPAR) α agonist fenofibrate suppresses chemically induced lung alveolar proliferative lesions in male obese hyperlipidemic miceInt. J. Mol. Sci.15(5)9160-9172(2014)