| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Ibudilast (formerly known as KC-404, AV-411 or MN-166) is a potent and nonspecific/nonselective inhibitor of the phosphodiesterase (PDE). It has been marketed in Japan for treating asthma. Ibudilast has antiinflammatory activity possibly due to the potent inhibition of PDE4. Ibudilast can be used as a bronchodilator, a vasodilator and/or a neuroprotective agent. It may also be useful in the treatment of multiple sclerosis because of its ability to inhibit platelet aggregation.
| ln Vitro |
Ibudilast (1~100 μM; 24 hours; microglia) significantly reduces TNF-α production at 10 and 100 μM and suppresses the production of IL-1β and IL-6 at 100 μM [1]. Neuronal cells treated with Ibudilast (1~100 μM; 48 hours) have a significantly higher rate of neuronal survival. Microglia treated with Ibudilast (1~100 μM; 48 hours) produce less superoxide and NO [1]. Ibudilast increases the synthesis of IL-10 in a dose-dependent way. Ibudilast raises GDNF and NT-4 mRNA expression in addition to NGF mRNA and protein levels. Ibudilast dose-dependently lessens the apoptotic alterations seen in neuronal cells [1].
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| ln Vivo |
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Microglia Tested Concentrations: 1~100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Suppressed both IL-1β and IL-6 production at 100 µM, and Dramatically suppresses TNF-α production at 10 and 100 µM. |
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| Animal Protocol |
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| References |
[1]. Mizuno T, et al. Neuroprotective role of phosphodiesterase inhibitor ibudilast on neuronal cell death induced by activated microglia. Neuropharmacology. 2004 Mar;46(3):404-11.
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| Molecular Formula |
C14H18N2O
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|---|---|
| Molecular Weight |
230.31
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| CAS # |
50847-11-5
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| Related CAS # |
Ibudilast-d7;2713301-45-0;Ibudilast-d7-1;1204192-90-4
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| SMILES |
CC(C)C(C1=C2C=CC=CN2N=C1C(C)C)=O
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| Chemical Name |
2-methyl-1-(2-propan-2-ylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one
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| Synonyms |
Ibudilast; AV-411, KC-404; KC 404; MN-166, AV 411, AV411, KC404; MN166, MN 166
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.67 mg/mL (11.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 26.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.67 mg/mL (11.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 26.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.67 mg/mL (11.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (10.85 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (10.85 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: 0.5 mg/mL (2.17 mM) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 7: ~2.7 mg/mL in 10% DMSO : 90% (20% SBE-β-CD in saline) ~2.7 mg/mL in 10% DMSO : 40% PEG300 : 5% Tween80 + : 45% saline ~2.7 mg/mL in 10% DMSO : 90% corn oil |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3420 mL | 21.7099 mL | 43.4197 mL | |
| 5 mM | 0.8684 mL | 4.3420 mL | 8.6839 mL | |
| 10 mM | 0.4342 mL | 2.1710 mL | 4.3420 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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