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编 号:F105457
分子式:C28H39N3O2
分子量:449.63
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10mM*1mL in DMSO
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2mg
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5mg
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10mg
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50mg
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生物活性:
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.

体内研究:
Nicodicosapent (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.

体外研究:
Nicodicosapent 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 IC50 value of 17 μM. Nicodicosapent significantly inhibits ApoB secretion in a dose-dependent manner with IC50 of 27 μM. Nicodicosapent results in a time-dependent hydrolysis in HepG2 cells.
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