178477 | ApoE4 Modulator, PH002 - Calbiochem

178477
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₇H₃₃N₅O₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      178477-10MG
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          Glass bottle 10 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          178477

          References

          Reference overview
          Chen, H., et al. 2011. J. Biol. Chem. 287, 5253.
          Brodbeck, J., et al. 2011. J. Bio. Chem. 286, 17217.
          Data Sheet

          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.