Pemafibrate

Pemafibrate may be used in research studies tostudy its effects on lipid metabolism, inflammation, and cardiovascular health.

Pemafibrate is an orally active, highly potent and selective peroxisome proliferator-activated receptor alpha (PPARα) agonist (hPPAR EC50 = 1 nM/α, 1.10 μM/γ, 1,58 μM/δ by cell-based reporter assays using respective transfectants). When administered in vivo Pemafibrate is >100-fold more effective than fenofibrate in lowering triglyceride (TG) in normal rats (1 mg/kg p.o.) and in increasing HDL-cholesterol (HDL-C) in human apoA-I (h-apoA-I) transgenic mice (3 mg/kg p.o.). Compared to other fibrates, pemafibrate′s distinct Y-shaped structure aids in stronger PPAR-α activation, better lipid binding, greater potency, and adaptability to structural changes caused by binding of coactivators. Pemafibrate shows anti-inflammatory activities like lowering the levels of interleukin-6, tumor necrosis factor-α, monocyte chemoattractant protein-1, vascular cell adhesion molecule-1 (VCAM-1), macrophage marker F4/80). It also exhibits antiatherogenic effects by lowering the levels of certain factors such as plasma triglycerides (TG), TG-rich lipoproteins, and apolipoprotein C-III (apoC-III), and increases lipoprotein lipase (LPL) activity and high-density lipoprotein (HDL) levels. Pemafibrate promotes fibroblast growth factor 21 and contributes to the reduction of insulin resistance.