Cas No.: | 836683-15-9 |
Synonyms: | BCT197;BCT-197;BCT 197 |
SMILES: | O=C(NC1CC1)C2=CC=C(C)C(N3N=CC(C(C4=CC=CC(C#N)=C4)=O)=C3N)=C2 |
Formula: | C22H19N5O2 |
M.Wt: | 385.42 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | 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)[1] |
In Vivo: | BCT197 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 BCT197 (75 mg on days 1 and 6) shows a marked improvement in lung function in COPD patients[2]. |
In Vitro: | Acumapimod is an inhibitor of p38α with an IC50 value of less than 1 μM. |
References: | [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. |