Ibudilast (Synonyms: AV 411,KC-404) |
Catalog No.GC13275
One-Click Copy Product Info
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inhibitor of PDE4
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonyms | AV 411,KC-404 | ||
| Chemical Name | 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 | ||
| Formula | C14H18N2O | M.Wt | 230.3 |
| Solubility | ≤25mg/ml in ethanol;16mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.3422 mL | 21.7108 mL | 43.4216 mL |
| 5 mM | 868.4 μL | 4.3422 mL | 8.6843 mL |
| 10 mM | 434.2 μL | 2.1711 mL | 4.3422 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)