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ChemicalBook--->CAS DataBase List--->1311174-68-1

1311174-68-1

1311174-68-1 Structure

1311174-68-1 Structure
IdentificationBack Directory
[Name]

PH002
[CAS]

1311174-68-1
[Synonyms]

PH002
PH-002
PH 002
PH-002 >=98% (HPLC)
PH002;PH-002;PH 002
4-[[4-[[2-(3,4-Dihydro-3-methyl-4-oxo-1-phthalazinyl)acetyl]amino]phenyl]methyl]-1-piperazinecarboxylic acid 1,1-dimethylethyl ester
1-Piperazinecarboxylic acid, 4-[[4-[[2-(3,4-dihydro-3-methyl-4-oxo-1-phthalazinyl)acetyl]amino]phenyl]methyl]-, 1,1-dimethylethyl ester
[Molecular Formula]

C27H33N5O4
[MDL Number]

MFCD22666400
[MOL File]

1311174-68-1.mol
[Molecular Weight]

491.58
Chemical PropertiesBack Directory
[storage temp. ]

Keep in dark place,Sealed in dry,2-8°C
[solubility ]

DMSO: soluble10mg/mL (clear solution)
[form ]

powder
[color ]

white to beige
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P280-P301+P312-P302+P352-P305+P351+P338
[WGK Germany ]

3
Hazard InformationBack Directory
[Uses]

PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.
[Biological Activity]

PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells th at restores mitochondrial cytochrome c oxidase subunit 1 levelsrescues impairments of mitochondrial motility and neurite outgrowth. PH-002 is an apoE4 structure corrector th at reverses the apoE4 detrimental effects.
[in vivo]

PH-002 is also shown to increase COX1 levels in primary neurons from NSE-apoE4 transgenic mouse cortex and hippocampus. After 4 days of treatment with PH-002 (200 nM), COX1 levels are increased by ~60%. PH-002 (100 nM) increases dendritic spine development in primary neurons from NSE-apoE4 transgenic mice to levels comparable with those in NSE-apoE3 primary neurons (apoE3-expressing primary neurons treated with PH-002 gave results identical to untreated primary neurons)[2].

[IC 50]

apoE
[References]

[1] Brodbeck J, et al. Structure-dependent impairment of intracellular apolipoprotein E4 trafficking and its detrimental effects are rescued by small-molecule structure correctors. J Biol Chem. 2011 May 13;286(19):17217-26. DOI:10.1074/jbc.M110.217380
[2] Chen HK, et al. Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons. J Biol Chem. 2012 Feb 17;287(8):5253-66. DOI:10.1074/jbc.M111.276162
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