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    AZD3839
    AZD3839

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1314
    CAS #: 1227163-84-9Purity ≥98%

    Description: AZD3839 (AZD-3839; AZD 3839) is a novel, potent and selective BACE1 (β-secretase) inhibitor with the potential for the treatment of Alzheimer disease. It inhibits BACE1 with a Ki of 26.1 nM and exhibits about 14-fold selectivity over BACE2. AZD3839 is clinical candidate for the treatment of Alzheimer disease. It inhibits BACE1 activity, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from mouse and guinea pig primary cortical neurons. AZD3839 exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate.

    References: J Biol Chem. 2012 Nov 30;287(49):41245-57; J Med Chem. 2012 Nov 8;55(21):9346-61.

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    Molecular Weight (MW)431.41
    FormulaC24H16F3N5
    CAS No.1227163-84-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: 86 mg/mL (199.3 mM)
    Solubility (In vivo)5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3: 2 mg/mL 
    SynonymsAZD3839; AZD-3839; AZD 3839


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    In Vitro

    In vitro activity: In SH-SY5Y cells, AZD3839 efficiently decreases the Aβ40 levels with IC50 of 4.8 nM, and decreases the formation of sAPPβ with IC50 of 16.7 nM. AZD3839 also decreases the Aβ40 levels secreted from C57BL/6 mouse primary cortical neurons, N2A cells, and Dunkin-Hartley guinea pig primary cortical neurons with IC50 values of 50.9, 32.2, and 24.8 nM, respectively. AZD3839 causes in vitro BACE1 inhibition in the cell assay with IC50 value of 16.7 nM.


    Kinase Assay: AZD3839 (free base) is a potent and selective BACE1 inhibitor with IC50 of 23.6 uM, about 14-fold selectivity over BACE2, also a β-secretase enzyme inhibitor. target: BACE1, β-secretase enzyme.


    Cell Assay: AZD3839 concentration-dependently inhibited BACE1 activity in a biochemical fluorescence resonance energy transfer assay, Aβ and sAPPβ release from modified and wild-type human SH-SY5Y cells and mouse N2A cells as well as from guinea pig and mouse primary cortical neurons. Selectivity against BACE2 and cathepsin D was 14 and >1000-fold, respectively.

    In VivoIn C57BL/6 mice, AZD3839 (69 mg/kg, p.o.) causes a dose- and time-dependent reduction of plasma and brain Aβ. In guinea pig and non-human primates, AZD3839 also inhibits Aβ generation.
    Animal modelC57BL/6 mice.
    Formulation & DosageDissolved in 5% dimethylacetamide and 20% hydroxypropyl-β-cyclodextrin in 0.3 M gluconic acid, pH 3, or 0.3 M gluconic acid, pH 3.; 69 mg/kg; p.o. administration
    ReferencesJ Biol Chem. 2012 Nov 30;287(49):41245-57; J Med Chem. 2012 Nov 8;55(21):9346-61. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    AZD3839

    Time- and dose-dependent inhibition of Aβ in C57BL/6 mice. J Biol Chem. 2012 Nov 30;287(49):41245-57.


     

    AZD3839

    Time- and dose-dependent inhibition of Aβ generation in guinea pig. J Biol Chem. 2012 Nov 30;287(49):41245-57.

    AZD3839

    Correlation between free plasma and free brain levels of AZD3839 in preclinical species. J Biol Chem. 2012 Nov 30;287(49):41245-57.


     

    AZD3839

    AZD3839 binding in the active site of BACE1, PDB ID code 4b05. J Biol Chem. 2012 Nov 30;287(49):41245-57. 

    AZD3839

    Time- and dose-dependent inhibition of Aβ generation in non-human primates. J Biol Chem. 2012 Nov 30;287(49):41245-57.


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