Fenofibric acid

Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC₅₀s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC₅₀ of 48 nM. IC50 & Target:EC50: 22.4 μM (PPARα), 1.47 μM (PPARγ), 1.06 μM (PPARδ)^[1]
IC50: 48 nM (COX-2)^[2] In Vitro: Fenofibric acid is a PPAR activitor, with EC₅₀s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively^[1]. Fenofibric acid (10, 25, 50, 75, and 100 nM) dose-dependently inhibits COX-2 enzyme, with IC₅₀ of 48 nM^[2]. Fenofibric acid (500 nM) reduces abundance of AOX1 protein in HepG2 cells^[3]. Fenofibric acid (100?μM) decreases JNK1/2, c-Jun, and p38 MAPK phosphorylation, and prevents the accumulation of reactive oxygen species, endoplasmic reticulum (ER) stress and disruption of blood retinal barrier (BRB) in response to the combination of high-glucose (HG) and hypoxia in ARPE-19 cells. Fenofibric acid (100?μM) activates IGF-IR/Akt/ERK1/2-mediated survival signaling pathways in ARPE-19 cells under HG conditions and hypoxia^[4]. In Vivo: Fenofibric acid (1, 5, 10 mg/kg, p.o.) shows anti-inflammatory activity in Wistar rats with acute inflammation induced by carrageenan^[2].