178477
ApoE4 Modulator, PH002
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 thereby reversing the detrimental effects of ApoE4.
别名:
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
登录 查看组织和合同定价。
选择尺寸
关于此项目
经验公式（希尔记法）:
C27H33N5O4
化学文摘社编号:
分子量:
491.58
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
N4(CCN(CC4)C(=O)OC(C)(C)C)Cc1ccc(cc1)NC(=O)C=C2NN(C(=O)c3c2cccc3)C
InChI key
HABKFQXKIOOEIG-UHFFFAOYSA-N
assay
≥99% (HPLC)
form
powder
potency
116 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL, clear, colorless
shipped in
wet ice
Quality Level
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
APOE4
APOE4
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Chen, H., et al. 2011. J. Biol. Chem.287, 5253.
Brodbeck, J., et al. 2011. J. Bio. Chem.286, 17217.
Brodbeck, J., et al. 2011. J. Bio. Chem.286, 17217.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持