MW-150 是一种选择性、CNS 渗透性和口服活性的 p38α MAPK 抑制剂,Ki 为 101 nM。它可抑制内源性 p38α MAPK 在活化的神经胶质中磷酸化内源性底物 MK2 的能力。
产品描述
MW-150 is a unique protein kinase inhibitor, is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM.
体外活性
MW-150 treatment blocked in a concentration-dependent manner the increased IL-1β production by activated glia. The IC50?values for these MW150 cellular activities are 332 nM (MK2) and 936 nM (IL-1β), values which are consistent with the in vitro?Ki?of 101 nM for p38αMAPK.
动物实验
MW-150 (2.5 mg/kg; given i.p.; daily for 14 days) treatment in APPNLh/NLh × PSP264L/P264L knock-in mouse (with no overexpression of the amyloid precursor protein) exhibits RAWM behavior indistinguishable from WT mice
Cas No.
1628502-91-9
分子式
C24H23N5
分子量
381.483
别名
MW01-18-150SRM
储存和溶解度
DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years