产品信息
抗原名称
p38 MAPK
商品描述
BMS-582949 is a potent and selective <b>p38 mitogen-activated protein kinase</b> (p38 MAPK) inhibitor with <b>IC50</b> of 13nM,inhibiting both p38 kinase activity and activation of p38.
分子量
406.48
纯度
99.05 %
可溶性
体外:
DMSO 81mg/mL(199.27mM)
Water <1mg/mL
Ethanol <1mg/mL
DMSO 81mg/mL(199.27mM)
Water <1mg/mL
Ethanol <1mg/mL
In vitro(体外研究)
BMS-582949 is found to inhibit p38 activation in cells, as measured by phosphorylation 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 is therefore a dual action p38 kinase inhibitor, inhibiting both p38 kinase activity and p38 activation in cells. 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(体内研究)
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.
背景
分子式
C22H26N6O2
CAS号
623152-17-0
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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