Apremilast (CC-10004)
(Synonyms: 阿普司特; CC-10004) 目录号 : GC10420
An orally available PDE4 inhibitor
Cas No.:608141-41-9
Sample solution is provided at 25 µL, 10mM.
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Apremilast, also known as CC-10004, is a novel and potent small-molecule inhibitor of phosphodiesterase 4 (PDE4), a key enzyme involved in cyclic adenosine monophosphate (cAMP) degradation and cytokine production of inflammatory cells. Apremilast binds to the catalytic site of PDE4, with values of inhibition constant IC50 and affinity constant Kiof 0.074 μM and 68 nM respectively, consequently leading to the degradation of cAMP. Apremilast exhibits anti-inflammatory activities against inflammatory disease in animal models as well as human chronic inflammatory diseases (such as psoriasis and psoriatic arthritis) by blocking the synthesis of a range of pro-flammatory cytokines and chemokines, including tumor necrosis factor alpha, interleukin 23, CXCL9 and CXCL10.
Reference
[1].Georg Schett, Victor S. Sloan, Randall M. Stevens and Peter Schafer. Apremilast: a novel PDE4 inhibitor in the treatment of autoimmune and inflammatory disease. Ther Adv Musculoskelet Dis. 2010; 2(5): 271-278
| Cell experiment [1]: | |
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Cell lines |
U937 human monocytic cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
18h; IC50=74 nM |
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Applications |
Apremilast was initially screened for PDE4 inhibition using a partially purified enzyme preparation from U937 human monocytic cells and which has been shown previously to contain predominantly PDE4B and PDE4D activities. Apremilast was also found to exhibit an IC50 of around 74 nM using 1 mM cAMP as substrate. |
| Animal experiment [1]: | |
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Animal models |
SCID mice |
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Dosage form |
5 mg·kg-1·day-1 ; oral taken |
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Applications |
The pharmacological activity of apremilast (5 mg·kg-1·day-1 total divided into 2 daily doses) was tested in comparison with cyclosporine (5 mg·kg-1·day-1 total divided into 2 daily doses) and vehicle control (0.1 mL·day-1 divided into twice daily doses) in a mouse xenograft model of psoriasis. Epidermal thickness and proliferation index correlated with histological findings and demonstrated significant differences between treatment groups. Notably, apremilast caused statistically significant reductions in epidermal thickness (P < 0.001) and proliferation index (P < 0.001). |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Schafer P H, Parton A, Gandhi A K, et al. Apremilast, a cAMP phosphodiesterase‐4 inhibitor, demonstrates anti‐inflammatory activity in vitro and in a model of psoriasis[J]. British journal of pharmacology, 2010, 159(4): 842-855. | |
| Cas No. | 608141-41-9 | SDF | |
| 别名 | 阿普司特; CC-10004 | ||
| 化学名 | N-[2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-1,3-dioxoisoindol-4-yl]acetamide | ||
| Canonical SMILES | CCOC1=C(C=CC(=C1)C(CS(=O)(=O)C)N2C(=O)C3=C(C2=O)C(=CC=C3)NC(=O)C)OC | ||
| 分子式 | C22H24N2O7S | 分子量 | 460.5 |
| 溶解度 | ≥ 23.05 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 10 mM | 0.2172 mL | 1.0858 mL | 2.1716 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet