BMS-582949 (hydrochloride)
Names
[ CAS No. ]:
912806-16-7
[ Name ]:
BMS-582949 (hydrochloride)
[Synonym ]:
unii-3z6gap3r9q
BMS-582949 (hydrochloride)
Biological Activity
[Description]:
BMS-582949 hydrochloride is a novel highly selective p38α MAPK inhibitor, inhibits p38α with IC50 of 13 nM. IC50 value: 13 nM[1]Target: p38αin 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 [2]. 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[1].
[Related Catalog]:
[References]
[Related Small Molecules]
SB203580
|
SB202190 (FHPI)
|
Doramapimod (BIRB 796)
|
LY2228820
|
SB 239063
|
Losmapimod
|
PD 169316
|
Talmapimod
|
Tat-NR2B9c
|
Dehydrocorydaline chloride
|
TAK-715
|
VX 702
|
VX-745
|
SKF 86002
|
Acumapimod
Chemical & Physical Properties
[ Molecular Formula ]:
C22H27ClN6O2
[ Molecular Weight ]:
442.94200
[ Exact Mass ]:
442.18800
[ PSA ]:
110.63000
[ LogP ]:
4.49520