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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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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
| 制备储备液 | |||
 |
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。