2. Metabolic Enzyme/Protease Apoptosis
  3. Phosphodiesterase (PDE) Apoptosis TNF Receptor
  4. Apremilast

Apremilast  (Synonyms: 阿普司特; CC-10004)

目录号: HY-12085 纯度: 99.91%
COA 产品使用指南

摩尔计算器

Apremilast (CC-10004) 是一种口服有效的磷酸二酯酶 4 (PDE4) 抑制剂，IC50 为 74 nM。Apremilast 抑制脂多糖 (LPS) 释放 TNF-α，IC50 为 104 nM。

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Apremilast Chemical Structure

Apremilast Chemical Structure

CAS No. : 608141-41-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥605
In-stock
1 mg ￥250
In-stock
5 mg ￥550
In-stock
10 mg ￥770
In-stock
25 mg ￥880
In-stock
50 mg ￥1100
In-stock
100 mg ￥1320
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Apremilast:

Apremilast 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].

IC50 & Target[1]

PDE4

74 nM (IC50)

体外研究
(In Vitro)

Apremilast (CC-10004) inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM (pIC50=6.98±0.2), which almost exactly replicates previous reported TNF-α inhibition by Apremilast on peripheral blood mononuclear cells (PBMCs) (IC50=110 nM) and which is similar to the potency of Apremilast for PDE4 enzymatic inhibition (IC50=74 nM). These results are clearly consistent with the hypothesis that Apremilast inhibits TNF-α by increasing intracellular cAMP levels. PKA, Epac1 and Epac2 knockdowns prevented TNF-α inhibition and IL-10 stimulation by Apremilast[1].

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

Apremilast 相关抗体:
体内研究
(In Vivo)

Apremilast (CC-10004), orally administered (5 mg/kg), significantly inhibits TNF-α production in the air pouch by 39 % (61±6 % of vehicle, P <0.001) and diminishes (by 28 %) the number of leukocytes present (72±12 % of vehicle, P<0.05). In agreement, immunohistologic analysis shows that neutrophil accumulation in the air pouch membrane is dramatically reduced by Apremilast. In the murine air pouch model, both Apremilast and methotrexate (MTX) significantly inhibit leukocyte infiltration, while Apremilast, but not MTX, significantly inhibits TNF-α release. The addition of MTX (1 mg/kg) to Apremilast (5 mg/kg) yields no more inhibition of leukocyte infiltration or TNF-α release than with Apremilast alone[1].
Apremilast is a novel, oral PDE4 inhibitor that has been shown to regulate inflammatory mediators. After oral administration of Apremilast, a mean maximum plasma concentration (Cmax) is found to be 67.00±14.87 ng/mL. The plasma concentration of Apremilast decreases rapidly and is eliminated from plasma with a terminal half-life of 0.92±0.46 h[2]

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

460.50

Formula

C22H24N2O7S
CAS 号
性状

固体

颜色

White to light yellow

中文名称

阿普司特
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 44 mg/mL (95.55 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1716 mL 10.8578 mL 21.7155 mL
5 mM 0.4343 mL 2.1716 mL 4.3431 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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

In Vivo:

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: ≥ 2.5 mg/mL (5.43 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.43 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

以下溶解方案，请直接配置工作液。建议现用现配，在短期内尽快用完。 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： 0.5% CMC-Na  0.5% Tween-80

    Solubility: 5 mg/mL (10.86 mM); Suspened solution; 超声助溶

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）。
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: 99.91%

COA (199 KB) LCMS (97 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

Raw 264.7 cells (100,000) are grown in 96-well plates. After 24 h, cells are stimulated with vehicle (final concentration of 0.025% DMSO) or with Apremilast at the indicated concentrations. After 30 minutes cells are stimulated with LPS 1 μg/mL for 4 h. When studying CGS21680 , SCH58261, ZM241385, BAY60-6583, or GS6201, the adenosine receptor ligands are added 15 minutes before Apremilast. Methotrexate is added 24 h and 1 h before Apremilast. Supernates are then collected and TNF-α levels are quantified with the Mouse TNF-α Quantikine ELISA Kit. IC50 (EC50) calculations are made using non-linear regression, sigmoidal dose-response, constraining the top to 100 % and bottom to 0 %, allowing variable slope, using GraphPad Prism v6.00[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1][2]

Mice[1]
Male mice are given weekly intraperitoneal injections of either MTX (1 mg/kg) or vehicle (PBS) for 4 weeks. Air pouches are generated by subcutaneous injection of 3 mL of sterile air and reinflated with 1.5 mL of sterile air 2 days later. Vehicle (0.5 % carboxymethylcellulose and 0.25 % Tween 80) or Apremilast (5 mg/kg) are orally dosed, with a syringe through a blunt-ended curved feeding tube, 24 h and 1 h before inflammation is induced on day 6 by injection of 1 mL of 2 % carrageenan suspension. Four hours later, mice are killed by CO2 narcosis, and exudates harvested with 2 mL PBS. Leukocytes are counted in a hemocytometer chamber and concentrations of cytokines are measured by ELISA or by the Luminex platform.
Rats[2]
Male Sprague Dawley rats (180-220 g) are used to study the pharmacokinetics of Apremilast. Diet is prohibited for 12 h before the experiment, but water is freely available. Blood samples (0.3 mL) are collected from the tail vein into heparinized 1.5 mL polythene tubes at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8 and 12 h after oral administration of Apremilast (6.0 mg/kg). The samples are immediately centrifuged at 4,000 g for 8 min. The plasma obtained (100 µL) is stored at −20°C until analysis. Plasma Apremilast concentration versus time data for each rat is analyzed by DAS (Drug and statistics) software.

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

Apremilast 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, 1 year; -20°C, 6 months。-80°C储存时，请在1年内使用， -20°C储存时，请在6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
DMSO 1 mM 2.1716 mL 10.8578 mL 21.7155 mL 54.2888 mL
5 mM 0.4343 mL 2.1716 mL 4.3431 mL 10.8578 mL
10 mM 0.2172 mL 1.0858 mL 2.1716 mL 5.4289 mL
15 mM 0.1448 mL 0.7239 mL 1.4477 mL 3.6193 mL
20 mM 0.1086 mL 0.5429 mL 1.0858 mL 2.7144 mL
25 mM 0.0869 mL 0.4343 mL 0.8686 mL 2.1716 mL
30 mM 0.0724 mL 0.3619 mL 0.7239 mL 1.8096 mL
40 mM 0.0543 mL 0.2714 mL 0.5429 mL 1.3572 mL
50 mM 0.0434 mL 0.2172 mL 0.4343 mL 1.0858 mL
60 mM 0.0362 mL 0.1810 mL 0.3619 mL 0.9048 mL
80 mM 0.0271 mL 0.1357 mL 0.2714 mL 0.6786 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:

Apremilast608141-41-9CC-10004阿普司特CC10004CC 10004Phosphodiesterase (PDE)ApoptosisTNF ReceptorTumor Necrosis Factor ReceptorTNFRorallyavailabletype-4cyclicnucleotidephosphodiesterasePDE-4,TNF-αlipopolysaccharideLPSPBMCInhibitorinhibitorinhibit

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