Ciprofibrate-d6 is intended for use as an internal standard for the quantification of ciprofibrate by GC- or LC-MS. Ciprofibrate is an agonist of peroxisome proliferator-activated receptor α (PPARα; EC50 = 0.9 ?M in a transactivation assay).1 It is selective for PPARα over PPARγ and PPARδ at 300 ?M.2 Ciprofibrate (250 ?M) induces cell cycle arrest at the G2/M and S phases in Fao rat, but not HepG2 human, hepatocellular carcinoma cells.3 It decreases fasting plasma levels of triglycerides and increases fasting plasma glucose levels in the apolipoprotein CIII transgenic mouse model of hypertriglyceridemia when administered at a dose of 10 mg/kg.4 Formulations containing ciprofibrate have been used in the treatment of hypertriglyceridemia.
1.Quang, T.H., Ngan, N.T.T., Minh, C.V., et al.Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldiiBioorg. Med. Chem. Lett.22(7)2527-2533(2012) 2.Forman, B.M., Chen, J., and Evans, R.M.Hypolipidemic drugs, polyunsaturated fatty acids, and eicosanoids are ligands for peroxisome proliferator-activated receptors α and δProc. Natl. Acad. Sci. USA94(9)4312-4317(1997) 3.Passilly, P., Jannin, B., Hassell, S.J., et al.Human HepG2 and rat Fao hepatic-derived cell lines show different responses to ciprofibrate, a peroxisome proliferator: analysis by flow cytometryExp. Cell. Res.223(2)436-442(1996) 4.Bighetti, E.J.B., Patricio, P.R., Casquero, A.C., et al.Ciprofibrate increases cholesteryl ester transfer protein gene expression and the indirect reverse cholesterol transport to the liverLipids Health Dis.850(2009)