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178477 ApoE4 Modulator, PH002 - Calbiochem

178477
Purchase on Sigma-Aldrich

Descripción

Replacement Information

Tabla espec. clave

Empirical Formula
C₂₇H₃₃N₅O₄

Products

Número de referenciaEmbalaje Cant./Env.
178477-10MG Frasco de vidrio 10 mg
Description
OverviewA 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.
Catalogue Number178477
Brand Family Calbiochem®
Synonyms4-{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
References
ReferencesChen, H., et al. 2011. J. Biol. Chem. 287, 5253.
Brodbeck, J., et al. 2011. J. Bio. Chem. 286, 17217.
Product Information
FormWhite powder
Hill FormulaC₂₇H₃₃N₅O₄
ReversibleY
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary TargetAPOE4
Primary Target IC<sub>50</sub>116 nM
Purity≥99% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

ApoE4 Modulator, PH002 - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

ApoE4 Modulator, PH002 - Calbiochem Certificados de análisis

CargoNúmero de lote
178477

Referencias bibliográficas

Visión general referencias
Chen, H., et al. 2011. J. Biol. Chem. 287, 5253.
Brodbeck, J., et al. 2011. J. Bio. Chem. 286, 17217.
Ficha técnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision09-July-2012 JSW
Synonyms4-{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
DescriptionA 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.
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityDMSO (100 mg/ml; clear, colorless solution)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesChen, H., et al. 2011. J. Biol. Chem. 287, 5253.
Brodbeck, J., et al. 2011. J. Bio. Chem. 286, 17217.