BMS-582949 (hydrochloride)

912806-16-7

C22H27ClN6O2

DMSO : >= 35 mg/mL (79.02 mM)

MAPK/ERK Pathway

BMS-582949 hydrochloride is an orally active and highly selective p38alpha MAPK inhibitor, with an IC₅₀ of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease^[1]. In Vitro: BMS-582949 displays a p38alpha IC₅₀ of 13 nM and a cellular TNFalpha IC₅₀ of 50 nM^[1].
BMS-582949 is a weak inhibitor of CYP3A4 BMS-582949 displays >2000-fold selectivity for p38alpha over a diverse panel of 57 kinases that include serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38gamma and delta isoforms^[1]. In Vivo: BMS-582949 (5-100 mg/kg, orally) is effective in both the acute murine model of inflammation and rat adjuvant arthritis model despite its slightly reduced potency^[1].