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178477 ApoE4 Modulator, PH002 - CAS 1311174-68-1 - Calbiochem

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 revers

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Synonyms: 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

Primary Target: APOE4
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178477
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Overview

Key Spec Table

CAS #Empirical Formula
1311174-68-1C₂₇H₃₃N₅O₄

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      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
      CAS number1311174-68-1
      FormWhite powder
      Hill FormulaC₂₇H₃₃N₅O₄
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetAPOE4
      Primary Target IC<sub>50</sub>116 nM
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      178477-10MG 04055977205176