Acumapimod
Based on 1 publication(s) in Google Scholar
Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.
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- Pureza: 99.68%
- No. CAS: 836683-15-9
- Fòrmula: C22H19N5O2
- Peso molecular:385.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Acumapimod
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Actividad biológica
IC50: less than 1 μM (p38α)[1]
Acumapimod is an inhibitor of p38α with an IC50 value of less than 1 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 836683-15-9
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Appearance Solid
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Peso molecular 385.42
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Fòrmula C22H19N5O2
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Color White to off-white
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SMILES
O=C(NC1CC1)C2=CC=C(C)C(N3N=CC(C(C4=CC=CC(C#N)=C4)=O)=C3N)=C2
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Synonyms
BCT197
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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J Pharmacol Exp Ther
Clinically Advanced p38 Inhibitors Suppress DUX4 Expression in Cellular and Animal Models of Facioscapulohumeral Muscular Dystrophy. [Abstract]2019 Aug;370(2):219-230. PMID: 31189728
Solvente y solubilidad
DMSO : ≥ 50 mg/mL (129.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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)
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: ≥ 2.5 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.49 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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Ficha de datos (272 KB)
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SDS (781 KB)
- English - EN (781 KB)
- Français - FR (781 KB)
- Deutsch - DE (781 KB)
- Norwegian - NO (781 KB)
- Español - ES (781 KB)
- Swedish - SV (781 KB)
- Italian - IT (781 KB)
- Korean - KR (781 KB)
- Portuguese - PT (781 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Norman P, et al. Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease. Expert Opin Investig Drugs. 2015 Mar;24(3):383-92. [Content Brief]
[2]. De Buck S, et al. Population PK-PD Model for Tolerance Evaluation to the p38 MAP Kinase Inhibitor BCT197. CPT Pharmacometrics Syst Pharmacol. 2015 Dec;4(12):691-700. [Content Brief]
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 | 2.5946 mL | 12.9729 mL | 25.9457 mL | 64.8643 mL |
| 5 mM | 0.5189 mL | 2.5946 mL | 5.1891 mL | 12.9729 mL | |
| 10 mM | 0.2595 mL | 1.2973 mL | 2.5946 mL | 6.4864 mL | |
| 15 mM | 0.1730 mL | 0.8649 mL | 1.7297 mL | 4.3243 mL | |
| 20 mM | 0.1297 mL | 0.6486 mL | 1.2973 mL | 3.2432 mL | |
| 25 mM | 0.1038 mL | 0.5189 mL | 1.0378 mL | 2.5946 mL | |
| 30 mM | 0.0865 mL | 0.4324 mL | 0.8649 mL | 2.1621 mL | |
| 40 mM | 0.0649 mL | 0.3243 mL | 0.6486 mL | 1.6216 mL | |
| 50 mM | 0.0519 mL | 0.2595 mL | 0.5189 mL | 1.2973 mL | |
| 60 mM | 0.0432 mL | 0.2162 mL | 0.4324 mL | 1.0811 mL | |
| 80 mM | 0.0324 mL | 0.1622 mL | 0.3243 mL | 0.8108 mL | |
| 100 mM | 0.0259 mL | 0.1297 mL | 0.2595 mL | 0.6486 mL |
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