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.
別名:
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
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この商品について
実験式（ヒル表記法）:
C27H33N5O4
CAS番号:
分子量:
491.58
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥99% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
Quality Segment
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
storage temp.
2-8°C
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
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)
保管分類
11 - Combustible Solids
一体何が起きているの？
WGK 3
引火点 (F)
Not applicable
引火点（°C）
Not applicable