Ibudilast
Based on 11 publication(s) in Google Scholar
Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.87%
- No. CAS: 50847-11-5
- Fòrmula: C14H18N2O
- Peso molecular:230.31
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ibudilast
More- Nat Commun. 2025 Sep 26;16(1):8477. [Abstract]
- Brain. 2023 Mar 1;146(3):898-911. [Abstract]
- Biomedicines. 2024 Apr 30;12(5):991. [Abstract]
- J Biol Chem. 2026 Jul 24;302(9):113357.
- Toxicol Appl Pharmacol. 2022 Aug 15:449:116112. [Abstract]
- Biochem Biophys Rep. 2025 Jun 26:43:102115. [Abstract]
- Addict Biol. 2025 Apr;30(4):e70033. [Abstract]
- Photochem Photobiol. 2016 Nov;92(6):816-825. [Abstract]
- Rapid Commun Mass Spectrom. 2024 Dec 15;38(23):e9916. [Abstract]
- Biomed Pharmacother. 2025 Nov:192:118638. [Abstract]
- bioRxiv. 2021 Apr 8.
Customer Validation & Images
-
WB
-
Cell Imaging/Staining
Actividad biológica
Descripciòn
IC50 & Target
phosphodiesterase[1]
In Vitro
Ibudilast (1~100 μM; 24 hours; microglia) suppresses both IL-1β and IL-6 production at 100 μM, and significantly suppresses TNF-α production at 10 and 100 μM[1].
Ibudilast (1~100 μM; 48 hours; neuronal cells) significantly increases the neuronal survival rate. Ibudilast (1~100 μM; 48 hours; microglia) inhibits the production of superoxide and NO[1].
Ibudilast upregulates the production of IL-10 in a dose-dependent manner. Ibudilast increases NGF mRNA and protein levels and GDNF and NT-4 mRNA expression. Ibudilast decreases the apoptotic changes observed in the neuronal cells in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Microglia
-
Concentration:1~100 μM
-
Incubation Time:24 hours
-
Result:Suppressed both IL-1β and IL-6 production at 100 µM, and significantly suppresses TNF-α production at 10 and 100 µM.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 50847-11-5
-
Appearance Solid
-
Peso molecular 230.31
-
Fòrmula C14H18N2O
-
Color White to off-white
-
SMILES
CC(C)C(C1=C2C=CC=CN2N=C1C(C)C)=O
-
Synonyms
KC-404; AV-411; MN-166
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Spatially-restricted inflammation-induced senescent-like glia in multiple sclerosis and patient-derived organoids. [Abstract]2025 Sep 26;16(1):8477. PMID: 41006208 -
Brain
2023 Mar 1;146(3):898-911. PMID: 35411386 -
Biomedicines
Characterization of a Clinically and Biologically Defined Subgroup of Patients with Autism Spectrum Disorder and Identification of a Tailored Combination Treatment. [Abstract]2024 Apr 30;12(5):991. PMID: 38790952 -
-
Toxicol Appl Pharmacol
2022 Aug 15:449:116112. PMID: 35688184 -
Biochem Biophys Rep
2025 Jun 26:43:102115. PMID: 40678798 -
Addict Biol
Ibudilast-Mediated Suppression of Neuronal TLR4 in the Prefrontal Cortex Mitigates Methamphetamine-Induced Neuroinflammation and Addictive Behaviours. [Abstract]2025 Apr;30(4):e70033. PMID: 40237256
Ibudilast purchased from MedChemExpress. Usage Cited in: Addict Biol. 2025 Apr;30(4):e70033. [Abstract]
Expression levels of TLR4, p‐NF‐κB and IL‐6 in the prefrontal cortex following treatment with 3 mg/kg and 10 mg/kg Ibudilast.
Ibudilast purchased from MedChemExpress. Usage Cited in: Addict Biol. 2025 Apr;30(4):e70033. [Abstract]
Expression of TLR4 in neurons, microglia and astrocytes following treatment with 3 and 10 mg/kg Ibudilast.
-
Photochem Photobiol
Resatorvid-based Pharmacological Antagonism of Cutaneous TLR4 Blocks UV-induced NF-κB and AP-1 Signaling in Keratinocytes and Mouse Skin. [Abstract]2016 Nov;92(6):816-825. PMID: 27859308 -
Rapid Commun Mass Spectrom
Equine metabolic investigation of the phosphodiesterase-4 inhibitor ibudilast as a potential performance enhancer. [Abstract]2024 Dec 15;38(23):e9916. PMID: 39307998 -
Biomed Pharmacother
Immune modulatory and vascular protective effects of Ibudilast in post-stroke inflammation. [Abstract]2025 Nov:192:118638. PMID: 41076947 -
Solvente y solubilidad
In Vitro:
DMSO : ≥ 140 mg/mL (607.88 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.67 mg/mL (11.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.67 mg/mL (11.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (2.17 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (282 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.3420 mL | 21.7099 mL | 43.4197 mL | 108.5493 mL |
| 5 mM | 0.8684 mL | 4.3420 mL | 8.6839 mL | 21.7099 mL | |
| 10 mM | 0.4342 mL | 2.1710 mL | 4.3420 mL | 10.8549 mL | |
| 15 mM | 0.2895 mL | 1.4473 mL | 2.8946 mL | 7.2366 mL | |
| 20 mM | 0.2171 mL | 1.0855 mL | 2.1710 mL | 5.4275 mL | |
| 25 mM | 0.1737 mL | 0.8684 mL | 1.7368 mL | 4.3420 mL | |
| 30 mM | 0.1447 mL | 0.7237 mL | 1.4473 mL | 3.6183 mL | |
| 40 mM | 0.1085 mL | 0.5427 mL | 1.0855 mL | 2.7137 mL | |
| 50 mM | 0.0868 mL | 0.4342 mL | 0.8684 mL | 2.1710 mL | |
| 60 mM | 0.0724 mL | 0.3618 mL | 0.7237 mL | 1.8092 mL | |
| 80 mM | 0.0543 mL | 0.2714 mL | 0.5427 mL | 1.3569 mL | |
| 100 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 1.0855 mL |
Ibudilast Related Classifications
HY-B0763 Related Classifications
Powered by Bioz