Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Purity: ≥98%
Acumapimod (also known as BCT197) is a potent and and orally bioavailable small molecule inhibitor of the p38 MAP kinase (MAPK-mitogen-activated protein kinase), with an IC50 for p38α of less than 1 μM. Numerous inflammatory mediators are produced under regulation by the p38 protein kinases, particularly p38α and p38β. For the treatment of a number of inflammatory conditions, including chronic obstructive pulmonary disease (COPD), BCT197 is currently being developed. Patients with COPD who take BCT197 intermittently for a short period of time (75 mg on days 1 and 6) notice a noticeable improvement in their lung function.
Targets |
p38α (IC50 < 1 μM)
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ln Vitro |
Acumapimod is a p38α inhibitor with a lower than 1 μM IC50 value.
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ln Vivo |
Acumapimod is an oral low-molecular-weight p38 inhibitor being developed for oral use to treat inflammatory conditions, such as chronic obstructive pulmonary disease (COPD) and other inflammatory diseases. Acumapimod (75 mg on days 1 and 6) is administered intermittently for a brief period of time and shows a significant improvement in lung function in COPD patients[2].
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Enzyme Assay |
Acumapimod is a p38α inhibitor with a lower than 1 μM IC50 value.
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Animal Protocol |
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References |
Molecular Formula |
C22H19N5O2
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Molecular Weight |
385.42
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Exact Mass |
385.15
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Elemental Analysis |
C, 68.56; H, 4.97; N, 18.17; O, 8.30
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CAS # |
836683-15-9
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Related CAS # |
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Appearance |
Yellow to orange solid powder
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SMILES |
CC1=C(C=C(C=C1)C(=O)NC2CC2)N3C(=C(C=N3)C(=O)C4=CC=CC(=C4)C#N)N
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InChi Key |
VGUSQKZDZHAAEE-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H19N5O2/c1-13-5-6-16(22(29)26-17-7-8-17)10-19(13)27-21(24)18(12-25-27)20(28)15-4-2-3-14(9-15)11-23/h2-6,9-10,12,17H,7-8,24H2,1H3,(H,26,29)
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Chemical Name |
3-[5-amino-4-(3-cyanobenzoyl)pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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: ≥ 2.5 mg/mL (6.49 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 25.0 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: ≥ 2.5 mg/mL (6.49 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 25.0 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: ≥ 2.5 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5946 mL | 12.9729 mL | 25.9457 mL | |
5 mM | 0.5189 mL | 2.5946 mL | 5.1891 mL | |
10 mM | 0.2595 mL | 1.2973 mL | 2.5946 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.
Median plasma concentration time profile of BCT197 after (a) a single dose administration (inset: log scale view), and (b) once daily dosing for 14 days. CPT Pharmacometrics Syst Pharmacol . 2015 Dec;4(12):691-700. td> |
Stochastic simulation of pharmacokinetics and corresponding drug effect in naïve healthy volunteer subjects (n = 500) treated with oral BCT197 given as (a,b) 75 mg single dose, (c,d) 25 mg on days 1, 6, and 10, and (e,f) 5.36 mg once daily for 14 days. CPT Pharmacometrics Syst Pharmacol . 2015 Dec;4(12):691-700. td> |