Overview

  • Product name

    AZD3839, BACE-1 inhibitor
  • Description

    Potent, selective, orally bioavailable  BACE-1 inhibitor
  • Alternative names

    • AZD3839
  • Biological description

    Potent and selective BACE-1 inhibitor (Ki = 26.1 nM), about 14-fold selectivity over BACE-2 (Ki = 372 nM). Decreases Aβ40 levels (IC50 = 4.8 nM) and decreases formation of sAPPβ (IC50 = 16.7 nM). Decreases Aβ40 levels secreted from C57BL/6 mouse primary cortical neurons, N2A cells, and Dunkin-Hartley guinea pig primary cortical neurons (IC50 values are 50.9, 32.2, and 24.8 nM respectively). In vitro BACE-1 inhibition (IC50 values are 16.7 nM and 50.9 nM in cell assay and for mouse primary cortical neurons respectively). Orally bioavailable, reduces brain Aβ40 levels in mouse and guinea pig models.

  • Purity

    > 99%
  • CAS Number

    1227163-84-9
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    (S)-3-(2-(Difluoromethyl)pyridin-4-yl)-7-fluoro-3-(3-(pyrimidin-5-yl)phenyl)-3H-isoindol-1-amine

  • Molecular weight

    431.41
  • Molecular formula

    C24H16F3N5
  • PubChem identifier

    46202416
  • Storage instructions

    Shipped at 4°C. Store at -20°C.
  • Solubility overview

    Soluble in DMSO and ethanol < 200 mM

  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    C1=CC(=CC(=C1)[C@@]2(C3=C(C(=CC=C3)F)C(=N2)N)C4=CC(=NC=C4)C(F)F)C5=CN=CN=C5
  • Source

    Synthetic

References

This product has been referenced in:

  • Aasa J  et al. Effect of solvents on the time-dependent inhibition of CYP3A4 and the biotransformation of AZD3839 in human liver microsomes and hepatocytes. Drug Metab Dispos 41:159-69 (2013). Read more (PubMed: 23073735) »
  • Swahn BM  et al. Design and synthesis of ß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction of ß-amyloid peptides. J Med Chem 55:9346-61 (2012). Read more (PubMed: 22924815) »
  • Jeppsson F  et al. Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease. J Biol Chem 287:41245-57 (2012). Read more (PubMed: 23048024) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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