Nicodicosapent

Nicodicosapent 是一种脂肪酸烟酸共轭体，可以抑制固醇调节元件结合蛋白 (SREBP) 的活性，调节胆固醇代谢的蛋白质如 PCSK9，HMG-CoA reductase，ATP citrate lyase 和 NPC1L1 等的活性。

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
2mg

￥1100.00

880.00

- +
5mg

￥1962.00

1570.00

- +
10mg

￥3262.00

2610.00

- +
50mg

￥9712.00

7770.00

- +
100mg

￥16025.00

12820.00

- +
200mg

￥0.00

0.00

- +
500mg

￥0.00

0.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajce57714
CAS: 1269181-69-2
别名:
分子式: C28H39N3O2
分子量: 449.63
纯度: >98%
溶解度: DMSO: ≥ 100 mg/mL (222.41 mM); Ethanol: 2 mg/mL (4.45 mM); Water: < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

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.

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[1].

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[1].

[1]. Vu CB, et al. Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid. J Med Chem. 2016 Feb 11;59(3):1217-31.