| Bioactivity | Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α. | ||||||||||||
| Target | IC50: less than 1 μM (p38α) | ||||||||||||
| Invitro | Acumapimod is an inhibitor of p38α with an IC50 value of less than 1 μM. | ||||||||||||
| In Vivo | Acumapimod is an oral low-molecular-weight p38 inhibitor currently in development for the treatment of several inflammatory conditions, including chronic obstructive pulmonary disease (COPD). Intermittent short-term dosing of Acumapimod (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients[2]. | ||||||||||||
| Name | Acumapimod | ||||||||||||
| CAS | 836683-15-9 | ||||||||||||
| Formula | C22H19N5O2 | ||||||||||||
| Molar Mass | 385.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [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. |