Molecular Formula | C22H26N6O2 |
Molar Mass | 406.48 |
Storage Condition | -20℃ |
In vitro study | BMS-582949 inhibition of p38 activation in the cell, reducing the level of phosphorylation of p38. When p38 is activated by LPS, BMS-582949 treatment rapidly reverses this activation, whereby p38 phosphorylation is reduced. BMS-582949 is a double-acting inhibitor of p38, which inhibits both the activity of p38 kinase itself and the activation of p38 itself in cells. BMS-582949 binds to p38a, causing a conformational change in the p38a activation loop (which can be phosphorylated by an upstream kinase), thereby inhibiting its phosphorylation. |
In vivo study | In mice, the clearance of BMS-582949 was 4.4/min/kg. After oral administration of 10 mg/kg BMS-582949, AUC0-8 h was 75.5 μm-h. The oral bioavailability BMS-582949 values were 90% in mice and 60% in rats. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.46 ml | 12.301 ml | 24.601 ml |
5 mM | 0.492 ml | 2.46 ml | 4.92 ml |
10 mM | 0.246 ml | 1.23 ml | 2.46 ml |
5 mM | 0.049 ml | 0.246 ml | 0.492 ml |