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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 Vitro 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 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 Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid
中文名称
Nicodicosapent
英文名称
Nicodicosapent
中文别名
尼古丁二十碳五烯酸
英文别名
Nicodicosapent | N-(2-((5Z,8Z,11Z,14Z,17Z)-Icosa-5,8,11,14,17-pentaenamido)ethyl)pyridine-3-carboxamide | Nicodicosapent [INN] | UNII-72995E50VA | AKOS040742302 | MS-28152 | 3-Pyridinecarboxamide, N-(2-(((5Z,8Z,11Z,14Z,17Z)-1-oxo-5,8,11,14,17-eicosapentae
CAS号
1269181-69-2
分子式
C28H39N3O2
分子量
449.63 g/mol
精确质量
≥98%
PSA
71.100 Ų
Logp
5.700
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Nicodicosapent 10mM in DMSO 1ml

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