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Beschreibung

A phthalazinone derived compound that directly binds to the 22-kDa amino-terminal region of apolipoprotein E4 (ApoE4) and blocks its intramolecular domain interactions in neuronal cells (IC50 = 116 nM) thereby reversing the detrimental effects of ApoE4. Established to be more potent than GIND25. Restores mitochondrial functions and elevates the levels of complex IV subunit 1. Shown to increase in COX1 levels in primary neurons from NSE-ApoE4 transgenic mouse cortex and hippocampus. Shown to rescue impairments of mitochondrial motility in primary neurons from NSE-ApoE4 transgenic mice (~ 200 nM). Also restores endoplasmic reticulum and Golgi apparatus transit of ApoE4 in cultured neurons and brings it to levels normally found in ApoE3 and ApoE4-R61T.