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    AZD1080
    AZD1080

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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 #: V0220
    CAS #: 612487-72-6Purity ≥98%

    Description: AZD1080 is a selective, potent, orally bioactive, and brain permeable GSK3 (glycogen synthase kinase-3) inhibitor with neuroprotective effects. It inhibits human GSK3α and GSK3β with Ki of 6.9 nM and 31 nM, respectively, also exhibits >14-fold selectivity for GSK3 over CDK2, CDK5, CDK1 and Erk2. AZD1080 has been reported to inhibit GSK3β by binding within the ATP pocket by means of the high resolution X-ray crystal structure. In addition, AZD1080 has been noted to suppression recombinant human GSK3α and GSK3β with the Ki values of 6.9 nM and 31 nM, respectively. AZD1080 inhibits tau phosphorylation in cells expressing human tau and in intact rat brain. 

    References: J Neurochem. 2013 May;125(3):446-56.

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    Molecular Weight (MW)

    334.37

    Formula

    C19H18N4O2

    CAS No.

    612487-72-6

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 52 mg/mL (155.5 mM)   

    Water: <1 mg/mL

    Ethanol: <1 mg/mL

    Solubility (In vivo)

    30% PEG400+0.5% Tween80+5% propylene glycol: 20 mg/mL 

    Synonyms

    AZD-1080; AZD-1080; AZD 1080; (Z)-3-(5-(morpholinomethyl)pyridin-2(1H)-ylidene)-2-oxoindoline-5-carbonitrile


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    In Vitro

    In vitro activity: AZD1080 is a selective, orally active, brain permeable GSK3 inhibitor, inhibits human GSK3α and GSK3β with a Ki of 6.9 nM and 31 nM, respectively, shows >14-fold selectivity against cdk2, cdk5, cdk1 and Erk2. AZD1080 inhibits tau phosphorylation in cells expressing human tau, with IC50 of 324 nM.

     

    Kinase Assay: GSK3 scintillation proximity assay is done. The competition experiments are carried out in duplicate with 10 concentrations of the inhibitor in clear-bottomed microtiter plates. The biotinylated peptide substrate biotin-AAEELDSRAGS(PO3H2)PQL, is added at a final concentration of 2 μM in an assay buffer containing 6 milliunits of recombinant human GSK3 (equal mix of both α and β), 12 mM MOPS, pH 7.0, 0.3 mM EDTA, 0.01% β-mercaptoethanol, 0.004% Brij 35, 0.5% glycerol, and 0.5 μg of bovine serum albumin/25 μl and preincubated for 10–15 min. The reaction is initiated by the addition of 0.04 μCi of [γ-33P]ATP and unlabeled ATP in 50 mM Mg(Ac)2 to a final concentration of 1 μM ATP and assay volume of 25 μl. Blank controls without peptide substrate are used. After incubation for 20 min at room temperature, each reaction is terminated by the addition of 25 μl of stop solution containing 5 mM EDTA, 50 μM ATP, 0.1% Triton X-100, and 0.25 mg of streptavidin-coated SPA beads corresponding to 35 pmol of binding capacity. After 6 h the radioactivity is determined in a liquid scintillation counter.

     

    Cell Assay: GSK3 scintillation proximity assay is done. The competition experiments are carried out in duplicate with 10 concentrations of the inhibitor in clear-bottomed microtiter plates. The biotinylated peptide substrate biotin-AAEELDSRAGS(PO3H2)PQL, is added at a final concentration of 2 μM in an assay buffer containing 6 milliunits of recombinant human GSK3 (equal mix of both α and β), 12 mM MOPS, pH 7.0, 0.3 mM EDTA, 0.01% β-mercaptoethanol, 0.004% Brij 35, 0.5% glycerol, and 0.5 μg of bovine serum albumin/25 μl and preincubated for 10–15 min. The reaction is initiated by the addition of 0.04 μCi of [γ-33P]ATP and unlabeled ATP in 50 mM Mg(Ac)2 to a final concentration of 1 μM ATP and assay volume of 25 μl. Blank controls without peptide substrate are used. After incubation for 20 min at room temperature, each reaction is terminated by the addition of 25 μl of stop solution containing 5 mM EDTA, 50 μM ATP, 0.1% Triton X-100, and 0.25 mg of streptavidin-coated SPA beads corresponding to 35 pmol of binding capacity. After 6 h the radioactivity is determined in a liquid scintillation counter.

    In Vivo

    AZD1080 inhibits tau phosphorylation in rat brain after oral dministration, with brain/plasma exposure ratio of 0.5 – 0.8 at peak concentrations. AZD1080 reverses cognitive deficits and rescues dysfunctional synapses in mice. Acute oral treatment with AZD1080 inhibits peripheral GSK3 activity, produces a dose-dependent reduction of the phosphorylated to total glycogen synthase (GS) ratio, with a mean maximal inhibitory effect of 49% at the highest dose (10 μmol/kg) at 2 h after dosing

    Animal model

    C57BL/6 mice

    Formulation & Dosage

    Dissolved in water with 0.5% ascorbic acid, 0.01% EDTA, pH 2.0; 3 or 10 μmol/kg, 6 mL/kg; Oral gavage

    References

    J Neurochem. 2013 May;125(3):446-56.


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

    AZD1080

    Binding, potency, and selectivity of AZD1080. J Neurochem. 2013 May;125(3):446-56

    AZD1080

    AZD1080 reverses MK-801-induced impairments in mouse model of cognition

    AZD1080

    Demonstration of peripheral target engagement in rats and in human


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