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^[1].

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.

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.

422.49

C₂₅H₂₂N₆O

1260248-03-0

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

• [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.
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