Cilomilast
(Synonyms: 西洛司特; SB-207499) 目录号 : GC17598
A PDE4 inhibitor
Cas No.:153259-65-5
Sample solution is provided at 25 µL, 10mM.
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Cilomilast, also known as SB-207499 or Ariflo, is a potent second generation inhibitor of type 4 phosphodiesterase (PDE4), an enzyme metabolizing cellular cyclic adenosine monophosphate (cAMP) which acts as a second messenger to disrupt the function of inflammatory cell and induce airway smooth muscle relaxation. Cilomilast is currently used for the treatment of chronic obstructive pulmonary disease (COPD) due to its strong anti-inflammatory activity as well as inhibitory effects against the release of neutrophil chemoattractants (such as tumor necrosis factor TNF- α, interleukin IL-8 and granulocyte-macrophage colony stimulating factor GM-CSF) and suppression of the recruitment of neutrophils into tissues and the LTB4 production.
Reference
[1].M Profita, G Chiappara, F Mirabella, RCDi Giorgi, L Chimenti, G Costanzo, L Riccobono, V Bellia, J Bousquet, and A M Vignola. Effect of cilomilast (Ariflo) on TNF-α, IL-8, and GM-CSF release by airway cells of patients with COPD. Thorax 2003; 58: 573-579
[2].Barry D. Zussman, Lisa J. Benincosa, Dawn M Webber, David j. Clark, Hugh Cowley, John Kelly, Robert D. Murdoch, James Upward, Peter Wyld, Andreas Port and Hermann Fuder. An overview of the pharmacokinetics of cilomilast (Ariflo), a new, orally active phosphodiesterase 4 inhibitor, in healthy young and elderly volunteers. J Clin Pharmacol 2001; 41: 950-958
| Cell experiment [1]: | |
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Cell lines |
MCS cell lines |
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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 |
11 d; 40 μM |
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Applications |
The results demonstrate that inhibition of PDE (Cilomilast) enhances ALP expression in MSCs via the cAMP pathway. The increase in the level of ALP activity is dependent on the dose of cilomilast. To study the effect of the inducers on MSC differentiation at similar proliferation rates, we treated MCSs, except those cultured in osteogenic medium, with 1% DMSO. We compared MSCs cultured for 11 days in the presence of different inducers with MSCs cultured in osteogenic medium in order to quantify the osteogenetic effects of the inducers. We found that the ALP activity levels of MCSs treated with a combination of PDE4 inhibitor (40 μM) and BMP-2 (300 ng/mL) were almost double the ALP activity level of MSCs treated with osteogenic medium, suggesting that the mineralisation process is more rapid. |
| Animal experiment [2]: | |
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Animal models |
Female C57BL/6 mice |
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Dosage form |
Cilomilast 0.05%; ocular surface instillation three times per day over a period of 7 days. |
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Applications |
Real-time PCR was used to quantify the expression of transcripts encoding IL-1α, IL-1β, and TNF-α in the corneas and conjunctivae of DED-induced mice. Treatment with topical cilomilast significantly decreased the corneal expression of TNF-α as compared with the vehicle-treated group. Compared with the DED-untreated corneas, treatment with cilomilast significantly reduced IL-1α and TNF-α expression. |
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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] Munisso M C, Kang J H, Tsurufuji M, et al. Cilomilast enhances osteoblast differentiation of mesenchymal stem cells and bone formation induced by bone morphogenetic protein 2[J]. Biochimie, 2012, 94(11): 2360-2365. [2] Sadrai Z, Stevenson W, Okanobo A, et al. PDE4 inhibition suppresses IL-17–associated immunity in dry eye disease[J]. Investigative ophthalmology & visual science, 2012, 53(7): 3584-3591. | |
| Cas No. | 153259-65-5 | SDF | |
| 别名 | 西洛司特; SB-207499 | ||
| 化学名 | 4-cyano-4-(3-cyclopentyloxy-4-methoxyphenyl)cyclohexane-1-carboxylic acid | ||
| Canonical SMILES | COC1=C(C=C(C=C1)C2(CCC(CC2)C(=O)O)C#N)OC3CCCC3 | ||
| 分子式 | C20H25NO4 | 分子量 | 343.42 |
| 溶解度 | ≥ 12.95 mg/mL in DMSO, ≥ 49.9 mg/mL in EtOH with ultrasonic and warming | 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 | 2.9119 mL | 14.5594 mL | 29.1189 mL |
| 5 mM | 0.5824 mL | 2.9119 mL | 5.8238 mL |
| 10 mM | 0.2912 mL | 1.4559 mL | 2.9119 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet