Gemfibrozil-d₆is intended for use as an internal standard for the quantification of gemfibrozil by GC- or LC-MS. Gemfibrozil is a peroxisome proliferator-activated reporter α (PPARα) and PPARγ agonist (EC₅₀s = 193.3 and 147.8 µM, respectively, in transactivation assays).¹In vivo, gemfibrozil (50 mg/kg, p.o.) reduces serum total cholesterol, triglyceride, and LDL levels in a rat model of high-cholesterol diet-induced hyperlipidemia.²Gemfibrozil (100 mg/kg per day) reduces atherosclerotic plaque area, superoxide production, and expression of the genes encoding the NF-κB subunit p65 and chemokine (C-C) motif ligand 2 (CCL2) inApoE^-/-mice.³Formulations containing gemfibrozil have been used in the treatment of high cholesterol.

1.Kim, N.J., Lee, K.O., Koo, B.W., et al.Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARα/γ dual agonistsBioorg. Med. Chem. Lett.17(13)3595-3598(2007) 2.Solanki, Y.B., and Jain, S.M.Antihyperlipidemic activity of Clitoria ternatea and Vigna mungo in ratsPharm. Biol.48(8)915-923(2010) 3.Calkin, A.C., Cooper, M.E., Jandeleit-Dahm, K.A., et al.Gemfibrozil decreases atherosclerosis in experimental diabetes in association with a reduction in oxidative stress and inflammationDiabetologia49(4)766-774(2006)