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 Aβ40 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.
For research use only. We do not sell to patients.
- CAS No.: 1146544-18-4
- Formula: C33H55N3O4
- Molecular Weight:557.81
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Cathepsin Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
BACE1 0.002 μM (IC50) |
Cathepsin D 0.001 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
24 μM
Compound: 14, NB-533
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Inhibition of BACE1 expressed in CHO cells expressing human recombinant APP assessed as amyloid beta40 aggregation
Inhibition of BACE1 expressed in CHO cells expressing human recombinant APP assessed as amyloid beta40 aggregation
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[PMID: 19195887] |
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. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:APP51/16 transgenic mice (expressing wild-type human APP under a brain-specific promoter)[1]
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Dosage:100 μmol/kg
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Administration:p.o.; at 0 and 3 hours
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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.
Chemical Information
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CAS No. 1146544-18-4
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Molecular Weight 557.81
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Formula C33H55N3O4
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Amyloid: Congo Red Amyloid Staining
Congo red amyloid staining is a histochemical method used to detect extracellular amyloid deposits in tissue sections based on the affinity of Congo red dye for β-pleated sheet-rich protein aggregates. When bound to amyloid, Congo red produces characteristic apple-green birefringence under polarized light microscopy, which is widely regarded as a diagnostic feature of amyloid deposition in histopathology. The diagnostic principle relies on the combination of dye binding (congophilia) and optical anisotropy under polarized illumination, which distinguishes amyloid from most non-amyloid eosinophilic extracellular deposits in routine histological evaluation. Amyloid identification by Congo red staining remains a cornerstone in diagnostic pathology despite the availability of adjunct methods such as immunohistochemistry and mass spectrometry, particularly because of its ability to localize deposits directly within tissue architecture. The specificity of Congo red-positive deposits is incre
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)