Description
Nicodicosapent is a fatty acid niacin conjugate that is also an inhibitor of the sterol regulatory element binding protein (SREBP), a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.In VitroNicodicosapent decreases the production of mature SREBP-2 protein in HepG2 cells, but does not interact with the GPR109A receptor. Nicodicosapent shows a synergistic inhibition on secreted PCSK9 and has an IC 50 value of 17 µM. Nicodicosapent significantly inhibits ApoB secretion in a dose-dependent manner with IC 50 of 27 µM. Nicodicosapent results in a time-dependent hydrolysis in HepG2 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoNicodicosapent (100 mg/kg po) produces high plasma levels of nicotinuric acid in the plasma. ApoE*3-Leiden mice treated with Nicodicosapent show a significant reduction in PCSK9 levels, LDL particles including VLDL and LDL cholesterol, as well as plasma triglycerides. MCE has not independently confirmed the accuracy of these methods. They are for reference only