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Art. -Nr.: HY-125405

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AZ3971

AZ3971 is an orally active, blood-brain barrier permeable BACE1 inhibitor that does not affect the activity of γ-secretase. AZ3971 reduces the production of Aβ. AZ3971 can be used for the research of Alzheimer's disease.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1260248-03-0
Formel: C₂₅H₂₂N₆O
Molecular Weight:422.49

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

AZ3971 Chemical Structure

CAS. Nr.: 1260248-03-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Beta-secretase Isoform-spezifische Produkte anzeigen :

BACE1
BACE2

In Vitro

AZ3971 potently blocks BACE1-mediated cleavage of APP with an IC₅₀ of 5.4 nM in SH-SY5Y cells^[1].
AZ3971 (5 hours) inhibits Aβ42 production with an IC₅₀ of 8.9 nM in HEK.APPswe cells after 5 hours of exposure^[1].
AZ3971 (overnight) blocks Aβ40 generation with an IC₅₀ of 37 nM in mPCNs after overnight exposure^[1].
AZ3971 (10 μM) does not inhibit γ-secretase activity in HEK cells expressing C99 when tested at 10 μM^[1].
AZ3971 (13-42 nM; 5 hours) produces an additive inhibitory effect on Aβ42 production when combined with AZ4800 in HEK.APPswe cells after 5 hours of exposure, without affecting AZ4800 (HY-120449) potency^[1].
AZ3971 (30-100 nM; overnight) produces an additive inhibitory effect on Aβ42 production when combined with AZ4800 in mPCNs after overnight exposure, without affecting AZ4800 potency^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AZ3971 (50-100 µmol/kg; p.o.; single dose) reduces brain Aβ42 levels in a dose-dependent manner, with a 30% reduction at 100 µmol/kg and a 23% reduction at 80 µmol/kg in female C57BL/6 mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6 (female, 8-week-old; female, 11-week-old)^[1]
Dosage:

50 µmol/kg; 80 µmol/kg; 100 µmol/kg
Administration:

p.o.; single dose
Result:

Reduced brain Aβ42 levels by 30% compared to vehicle at 100 µmol/kg.
Reduced brain Aβ42 levels by 23% and brain Aβ40 levels by 19% compared to vehicle at 80 µmol/kg.
Achieved free brain concentrations of 44±17 nM following 80 µmol/kg single dose.

Chemical Information

CAS. Nr. 1260248-03-0
Molecular Weight 422.49
Formel C₂₅H₂₂N₆O
SMILES

NC1=N[C@](C=2C1=NC=CN2)(C3=CC(C)=C(OC)C(C)=C3)C4=CC(=CC=C4)C=5C=NC=NC5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Strömberg K, et al. Combining an amyloid-beta (Aβ) cleaving enzyme inhibitor with a γ-secretase modulator results in an additive reduction of Aβ production. FEBS J. 2015 Jan;282(1):65-73.
[Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biologische Aktivität
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- In Vitro
- In Vivo
Chemical Information
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AZ3971

Alle Beta-secretase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

AZ3971 Related Classifications

HY-125405 Related Classifications