Fenofibric acid (FNF acid) is the active form of fenofibrate, a synthetic phenoxy-isobutyric acid derivate with antihyperlipidemic activity.

PPARα:22.4 µM(EC50), PPARδ:1.06 µM(EC50), PPARγ:1.47 µM(EC50), COX-2:48 nM

Fibric acids, active forms of fibrate drugs and activators of peroxisome proliferator-activated receptor-alpha (PPARα), are also known for an HDL-raising effect. Fibric acids enhance fatty acid catabolism and accordingly reduce plasma lipid level, predominantly triglyceride (TG). Fenofibric acid increases the expression of ABCA1 and apoA-I–mediated HDL production. The effect on ABCA1 expression was through the enhancement of the transcription of the ABCA1 gene being dependent on LXR[1].

Fenofibric acid attenuates aberrant increases of circulating EPC(Endothelial Progenitor Cells) in OIR mice. Inhibitory effect of Fenofibric acid on EPC mobilization in the OIR model is PPARα-dependent.Fenofibric acid Inhibits hypoxia-induced retinal EPC increase in a PPARα-dependent manner. Fenofibric acid decreases CXCR4-positive EPC in the circulation, downregulates the serum SDF-1 level and suppresses HIF-1a and SDF-1 overexpression in the retina[1].

PPAR activators fenofibric acid is dissolved in DMSO and added to the culture medium containing 0.2% BSA. RAW264 cells are washed with PBS and cultured an additional 48 hours in the presence of fenofibric acid in DMEM/F-12(1:1) medium containing 2% TCM and 0.2% BSA. During the last 24 hours of the drug treatment, 300 mol/L of dibutyryl cAMP and apoA-I (10 μg/mL) are added to the medium. THP-1 cells are also treated with the compound and apoA-I in 0.2% BSA-RPMI 1640 medium and 0.1% BSA-MEM. Cholesterol and choline-phospholipid released into the medium by apoA-I are determined enzymatically. Adherent cells are dissolved in 0.1 N NaOH for protein determination by bicinchoninic acid protein assay system. (Only for Reference)