| Identification | Back 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 Properties | Back 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 | [InChI]
1S/C27H33N5O4/c1-27(2,3)36-26(35)32-15-13-31(14-16-32)18-19-9-11-20(12-10-19)28-24(33)17-23-21-7-5-6-8-22(21)25(34)30(4)29-23/h5-12H,13-18H2,1-4H3,(H,28,33) | [InChIKey]
GSXXTLWPQMHHDJ-UHFFFAOYSA-N | [SMILES]
O=C(N1CCN(CC2=CC=C(NC(CC3=NN(C)C(C4=C3C=CC=C4)=O)=O)C=C2)CC1)OC(C)(C)C |
| Hazard Information | Back 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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| Company Name: |
Twochem Co.Ltd.
|
| Tel: |
021-58111628 15800915896 |
| Website: |
cn.twochem.com |
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
|