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编 号:F621496
分子式:C24H24ClN5
分子量:417.93
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生物活性:
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.

体内研究:
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) (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 hydrochloride (MW01-18-150SRM hydrochloride) (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.Animal Model:APP/PS1 transgenic (Tg) mouse (overexpresses amyloid-beta)
Dosage:2.5 mg/kg
Administration:Oral daily; 3-4 months (until cognitive impairment is present)
Result:Improved the Tg mice performance in both cognitive tests.

体外研究:
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits in a concentration-dependent manner the ability of the endogenous p38αMAPK to phosphorylate an endogenous substrate MK2 in activated glia. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) 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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