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BMS-582949 inhibits both p38 kinase activity and activation of p38. BMS-582949 treatment of cells in which p38 has been activated by LPS rapidly reversed p38 activation as shown by loss of phosphorylation of p38. BMS-582949 binding to p38a results in a conformational change of the activation loop which is phosphorylated by upstream kinases, therefore it inhibits phosphorylation of p38 by upstream MKK by inducing a less accessible conformation of the activation loop.
In vivo, the mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively.
Molecular Weight | 406.48 |
Formula | C22H26N6O2 |
CAS Number | 623152-17-0 |
Solubility (25°C) | DMSO: ≥ 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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