Acumapimod (also known as BCT197) is a potent and orally bioavailable small molecule inhibitor of the p38 MAP kinase (MAPK-mitogen-activated protein kinase) with an IC50 of less than 1 μM for p38α. The p38 protein kinases such as p38α and p38β regulate the production of multiple inflammatory mediators. BCT197 is currently in development for the treatment of several inflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-term dosing of BCT197 (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients.
理化性质和储存条件
| Molecular Weight (MW) | 385.42 |
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| Formula | C22H19N5O2 |
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| CAS No. | 836683-15-9 |
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| Storage | -20℃ for 3 years in powder form |
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| -80℃ for 2 years in solvent |
| Solubility (In vitro) | DMSO: 10 mM |
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| Water: <1 mg/mL |
| Ethanol: |
| SMILES Code | O=C(NC1CC1)C2=CC=C(C)C(N3N=CC(C(C4=CC=CC(C#N)=C4)=O)=C3N)=C2 |
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| Chemical Name | 3-(5-amino-4-(3-cyanobenzoyl)-1H-pyrazol-1-yl)-N-cyclopropyl-4-methylbenzamide |
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| Synonyms | BCT197A2201; Acumapimod; BCT-197; BCT197; BCT 197 |
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| InChi Key | VGUSQKZDZHAAEE-UHFFFAOYSA-N |
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实验参考方法
| In Vitro | In vitro activity: Acumapimod (also known as BCT197) is a potent and orally bioavailable small molecule inhibitor of the p38 MAP kinase (MAPK-mitogen-activated protein kinase) with an IC50 of less than 1 μM for p38α. The p38 protein kinases such as p38α and p38β regulate the production of multiple inflammatory mediators. BCT197 is currently in development for the treatment of several inflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-term dosing of BCT197 (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients.
Kinase Assay: Acumapimod is a p38α inhibitor with IC50 value of less than 1 μM.
Cell Assay: |
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| In Vivo | BCT197 is an orally bioactive small molecule inhibitor of MAPK p38 that is currently in development for the treatment of several inflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-term dosing of BCT197 (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients |
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| Formulation & Dosage |
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| References | CPT Pharmacometrics Syst Pharmacol. 2015 Dec;4(12):691-700; Expert Opin Investig Drugs. 2014 Aug;23(8):1067-77. |
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