Pemafibrate is an 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) innormal rats (1 mg/kg p.o.) and in increasing HDL-cholesterol (HDL-C) in humanapoA-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 tostructural 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.
Application：
Pemafibrate may be used in research studies tostudy its effects on lipid metabolism, inflammation, and cardiovascular health.
Biochem/physiol Actions：
Orally active, highly potent and selective peroxisome proliferator-activated receptor alpha (PPARα) agonist with >100-fold in vivo efficacy than fenofibrate.
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.).
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