ApoE4 Modulator, PH002

ApoE4 Modulator, PH002
4-{4-[2-(3-methyl-4-oxo-3,4-dihydro-phthalazin-1-yl)-acetylamido]-benzyl}-piperazine-1-carboxylic acid tert-butyl ester, ApoE4 Structure Corrector, PH-002, Apolipoprotein E4 structure corrector
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.
产品信息
Form  White powder
Primary Target  APOE4
Primary Target IC50  116 nM
Molar mass  491.58
Protect from Light  是的
Packaged under inert gas  是的
Cell permeable  是的
Reversible  是的
Purity  ≥99% by HPLC
Solubility  DMSO
商店和运输信息
Storage  +2°C to +8°C
Ship  Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling