Nicodicosapent (C09-1156-888)

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.Form:Solid. Specification: 0.98 Molecular Formula: C28H39N3O2 Molecular Weight: 449.63 PubChem CID: 50991753 Isomeric SMILES: CC/C=C/C/C=C/C/C=C/C/C=C/C/C=C/CCCC(=O)NCCNC(=O)C1=CN=CC=C1