BMS-582949 hydrochlorideCAS号： 912806-16-7分子式： C22H27ClN6O2分子量： 442.94描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease.
|
| 纯度 |
98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
|
| 基本信息 | |
| 别名 |
BMS-582949 HCl
|
| 可溶性/溶解性 |
DMSO : 25 mg/mL (56.44 mM; Need ultrasonic)
|
| 生物活性 | |
| 靶点 |
p38α MAPK；TNFα
|
| In vitro(体外研究) |
BMS-582949 displays a p38α IC50 of 13 nM and a cellular TNFα IC50 of 50 nM.
BMS-582949 is a weak inhibitor of CYP3A4 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. |
| In vivo(体内研究) |
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.
|
分子结构图
