MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a potent and selective inhibitor of p38α MAPK, with a Ki value of 101 nM. It exhibits excellent CNS penetration and oral bioavailability. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) effectively suppresses the phosphorylation of MK2, a substrate of endogenous p38α MAPK, in activated glial cells.

p38α:101 nM (Ki)

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[1]. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) blocks in a concentration-dependent manner the increased IL-1β production by activated glia. The IC 50 values are 332 nM and 936 nM for MK2 and IL-1β, respectively[1].

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[1]. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) (2.5 mg/kg; given i.p.; daily for 14 days) treatment in APP NLh/NLh × PS P264L/P264L knock-in mouse (with no overexpression of the amyloid precursor protein) exhibits RAWM behavior indistinguishable from WT mice[1]. Animal Model: APP/PS1 transgenic (Tg) mouse (overexpresses amyloid-beta)[1]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.