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编 号:F622317
分子式:C24H29Cl2N5O2
分子量:490.43
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生物活性:
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.

体内研究:
MW-150 dihydrochloride dihydrate (2.5 mg/kg; oral daily for 3?4 months) improves the APP/PS1 transgenic (Tg) mice performance in radial arm water maze (RAWM) and contextual fear conditioning tests.MW-150 dihydrochloride dihydrate (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.

体外研究:
MW-150 dihydrochloride dihydrate inhibits in a concentration-dependent manner the ability of the endogenous p38αMAPK to phosphorylate an endogenous substrate MK2 in activated glia. MW-150 dihydrochloride dihydrate blocks in a concentration-dependent manner the increased IL-1β production by activated glia. The IC50 values are 332 nM and 936 nM for MK2 and IL-1β, respectively.
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