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.
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- No. CAS: 1260248-03-0
- Fòrmula: C25H22N6O
- Peso molecular:422.49
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 8-week-old; female, 11-week-old)[1]
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Dosage:50 µmol/kg; 80 µmol/kg; 100 µmol/kg
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Administration:p.o.; single dose
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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
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No. CAS 1260248-03-0
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Peso molecular 422.49
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Fòrmula C25H22N6O
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SMILES
NC1=N[C@](C=2C1=NC=CN2)(C3=CC(C)=C(OC)C(C)=C3)C4=CC(=CC=C4)C=5C=NC=NC5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AZ3971 Related Classifications
HY-125405 Related Classifications
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