1. Neuronal Signaling Metabolic Enzyme/Protease
  2. Beta-secretase Cathepsin Amyloid-β
  3. NB-533

NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces 40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease.

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NB-533

NB-533 Chemical Structure

CAS No. : 1146544-18-4

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Description

NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces 40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease[1].

IC50 & Target[1]

BACE1

0.002 μM (IC50)

Cathepsin D

0.001 μM (IC50)

In Vitro

NB-533 potently inhibits human BACE-1 enzyme with an IC50 of 0.002 μM[1].
NB-533 inhibits Aβ40 release from human APP-transfected CHO cells with an IC50 of 0.024 μM[1].
NB-533 inhibits human cathepsin D with an IC50 of 0.001 μM[1].
NB-533 has an efflux ratio (BA/AB) of 9.4 in MDCK mdr1a cells, showing reduced P-glycoprotein susceptibility[1].

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

In Vivo

NB-533 (100 μmol/kg; p.o.; double-dose at 0 and 3 h) significantly reduces forebrain C99 by 20% and CSF Aβ40 by 26% in APP51/16 transgenic mice[1].

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

Animal Model: APP51/16 transgenic mice (expressing wild-type human APP under a brain-specific promoter)[1]
Dosage: 100 μmol/kg
Administration: p.o.; at 0 and 3 hours
Result: Reached brain levels of 0.53 μmol/kg, with no detectable effect on measured endpoints.
Reached brain levels of 1.5 μmol/kg, resulting in a significant 20% reduction in forebrain C99 and a significant 26% reduction in CSF Aβ40; no significant reduction in brain Aβ40 was observed.
Molecular Weight

557.81

Formula

C33H55N3O4

CAS No.
SMILES

O[C@@H]([C@@]1([H])NC([C@@H](N(C(CCCCCCCC[C@H](C1)C)=O)C)C)=O)CN[C@@H]2C3=CC(C(C)C)=CC=C3OC(C)(C2)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
NB-533
Cat. No.:
HY-182429
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