Ibudilast
(Synonyms: 异丁司特; KC-404; AV-411; MN-166) 目录号 : GC13275
An inhibitor of PDE4
Cas No.:50847-11-5
Sample solution is provided at 25 µL, 10mM.
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IC50: 54-239 nM
Ibudilast is an inhibitor of PDE4.
Phosphodiesterases (PDEs) are critical inflammation and wound healing modulators. Specific targeting of PDEs for the treatment of various diseases, such as chronic obstructive pulmonary disease (COPD), has been investigated.
In vitro: Ibudilast could potently inhibit purified human PDE4A, 4B, 4C and 4D with IC50 values at 54, 65, 239 and 166 nM, respectively. Ibudilast was also able to effectively block LPS-induced tumor necrosis factor and N-formyl-MetLeu-Phe-induced leukotriene B4 biosynthesis in human whole blood [1].
In vivo: Rats received a daily oral administration of 10, 30 or 60 mg/kg ibudilast. Results showed that in the vehicle-treated animals, white matter lesions and microglial activation occurred in the optic tract, internal capsule and corpus callosum. A low dose of ibudilast failed to suppress the white matter lesions and microglial activation, whereas a dose of either 30 or 60 mg/kg ibudilast ameliorated these lesions [2].
Clinical trial: Ibudilast was studied in 13 asthmatics for its effect on airway hypersensitivity to histamine inhalation. The PC20 values improved significantly following the initial treatment with ibudilast. In addition, the severity of the attacks decreased significantly. Improvements in the PC20 and asthmatic symptoms also were observed in the disodium chromoglycate group, but these were equal to or lesser than those in the ibudilast group [3].
References:
[1] Huang, Z. ,Liu, S.,Zhang, L., et al. Preferential inhibition of human phosphodiesterase 4 by ibudilast. Life Sciences 78(23), 2663-2668 (2006).
[2] Wakita H, Tomimoto H, Akiguchi I, Lin JX, Ihara M, Ohtani R, Shibata M. Ibudilast, a phosphodiesterase inhibitor, protects against white matter damage under chronic cerebral hypoperfusion in the rat. Brain Res. 2003 Nov 28;992(1):53-9.
[3] Kawasaki A, Hoshino K, Osaki R, Mizushima Y, Yano S. Effect of ibudilast: a novel antiasthmatic agent, on airway hypersensitivity in bronchial asthma. J Asthma. 1992;29(4):245-52.
| Cas No. | 50847-11-5 | SDF | |
| 别名 | 异丁司特; KC-404; AV-411; MN-166 | ||
| 化学名 | 2-methyl-1-[2-(1-methylethyl)pyrazolo[1,5-a]pyridin-3-yl]-1-propanone | ||
| Canonical SMILES | CC(C)C1=NN(C=CC=C2)C2=C1C(C(C)C)=O | ||
| 分子式 | C14H18N2O | 分子量 | 230.3 |
| 溶解度 | ≤25mg/ml in ethanol;16mg/ml in DMSO;20mg/ml in dimethyl formamide | 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 | 4.3422 mL | 21.7108 mL | 43.4216 mL |
| 5 mM | 0.8684 mL | 4.3422 mL | 8.6843 mL |
| 10 mM | 0.4342 mL | 2.1711 mL | 4.3422 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