BMS-582949 hydrochloride
CAS No. | 912806-16-7 | Cat. No. | BCP17651 |
Name | BMS-582949 hydrochloride | ||
Synonyms | BMS 582949 hydrochloride;BMS582949 hydrochloride; | ||
Formula | C22H27ClN6O2 | M. Wt | 442.94 |
Description | in vitro: BMS-582949 does not significantly inhibit cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 with IC50values >40 μM. It is a weak inhibitor of CYP3A4, with an IC50 value ranging from 18 to 40 μM based in multiple tests. BMS-582949 displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. BMS-582949 is also 450-fold selective over Jnk2, a MAP kinase involved in inflammation, and 190-fold selective over Raf[1].BMS-582949 is a novel highly selective p38α MAPK inhibitor. in vivo: The mouse clearance rate for BMS-582949 is 4.4 mL/min/kg. And, at an oral dose of 10 mg/kg, the mouse AUC0?8 h for BMS-582949 is 75.5 μM·h. BMS-582949 exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively. | ||
Pathways | MAPK Pathway | ||
Targets | p38 MAPK |
Structure
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