2. Metabolic Enzyme/Protease Autophagy
  3. Fatty Acid Synthase (FASN) Autophagy
  4. 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。

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Nicodicosapent Chemical Structure

Nicodicosapent Chemical Structure

CAS No. : 1269181-69-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1650
In-stock
2 mg ￥570
In-stock
5 mg ￥1500
In-stock
10 mg ￥2700
In-stock
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

Nicodicosapent 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

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.

体外研究
(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 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Nicodicosapent 相关抗体:
体内研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

449.63

Formula

C28H39N3O2
CAS 号
性状

固液混合物

颜色

Yellow to brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 100 mg/mL (222.41 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : 3.33 mg/mL (7.41 mM; 超声助溶)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2241 mL 11.1203 mL 22.2405 mL
5 mM 0.4448 mL 2.2241 mL 4.4481 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.75 mg/mL (8.34 mM); 澄清溶液

    此方案可获得 ≥ 3.75 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 37.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.79%

COA (275 KB) HNMR (489 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献
Animal Administration
[1]

Male Sprague-Dawley rats (n=4/treatment group) are administered with a single oral dose of either niacin (30 mg/kg) or Nicodicosapent (100 mg/kg). Compounds are formulated as an aqueous emulsion using Tween, Peceol, PEG400, and tocopherol. Nicodicosapent (170 mg) is formulated in 2.38 g of the oil mixture containing 40% Tween, 50% Peceol, 10% PEG400, and 0.2% tocopherol. The concentration of 5 in oil is 66 mg/g of oil. For oral dosing, this oil formulation is then diluted with 14.25 mL of water to form a 10 mg/mL drug emulsion and dosed as an oral gavage. Collection time points are 5, 15, and 30 min 1, 2, 4, 6, and 8 h postdose. Blood samples are collected via saphenous vein and placed in tubes containing paraoxon (10 μL of a 200 μM solution in DMSO) and stored on an ice block until centrifuged at 8000 rpm for 6 min at 2-8°C. The resulting plasma is kept frozen at −80°C until analysis. Nicodicosapent, nicotinic acid, and nicotinuric acid standard curves are generated to allow for quantitative analysis of plasma samples. Standard curves are generated by adding 10 μL of a given compound in methanol (50 μg/mL) to 50 μL of blank plasma in a 96-well microplate, resulting in the following final concentration range: 8333, 2083, 521, 130.2, 32.5, 8.1, 2.0, and 0.5 ng/mL. Then 300 μL of acetonitrile containing 100 ng/mL of an internal standard is added to each sample. The 96-well microplate is vortexed for 30 s and is then centrifuged for 45 min at 2300 g. Then 100 μL of supernatant is transferred from each sample to an empty 96-well microplate for analysis by LC/MS/MS. The instrument used is an Agilent liquid chromatograph equipped with a binary pump (1200 series), an autosampler (1200 series), and a degasser (1200 series). Mass spectrometric analysis is performed using an Agilent 6410 triple quadrupole with an ESI interface. The data acquisition and quantitation is done with Agilent Masshunter software. The column used is a Phenomenex Gemini C6 Phenyl 110A 50 mm×4.6 mm, 1.8 μm. The following mobile phase gradient is used (water = solvent A; methanol = solvent B): 0.01 min=45%A/55%B; 0.5 min=45%A/55%B; 1 min=5%A/95%B; 3.5 min=5%A/95%B; 3.51 min=45%A/55%B; 4 min=45%A/55%B.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Nicodicosapent 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.2241 mL 11.1203 mL 22.2405 mL 55.6013 mL
5 mM 0.4448 mL 2.2241 mL 4.4481 mL 11.1203 mL
DMSO 10 mM 0.2224 mL 1.1120 mL 2.2241 mL 5.5601 mL
15 mM 0.1483 mL 0.7414 mL 1.4827 mL 3.7068 mL
20 mM 0.1112 mL 0.5560 mL 1.1120 mL 2.7801 mL
25 mM 0.0890 mL 0.4448 mL 0.8896 mL 2.2241 mL
30 mM 0.0741 mL 0.3707 mL 0.7414 mL 1.8534 mL
40 mM 0.0556 mL 0.2780 mL 0.5560 mL 1.3900 mL
50 mM 0.0445 mL 0.2224 mL 0.4448 mL 1.1120 mL
60 mM 0.0371 mL 0.1853 mL 0.3707 mL 0.9267 mL
80 mM 0.0278 mL 0.1390 mL 0.2780 mL 0.6950 mL
100 mM 0.0222 mL 0.1112 mL 0.2224 mL 0.5560 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nicodicosapent1269181-69-2Fatty Acid Synthase (FASN)AutophagyInhibitorinhibitorinhibit

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