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.
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- No. CAS: 1146544-18-4
- Fòrmula: C33H55N3O4
- Peso molecular:557.81
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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
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Actividad biológica
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BACE1 0.002 μM (IC50) |
Cathepsin D 0.001 μM (IC50) |
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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] |
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.
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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No. CAS 1146544-18-4
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Peso molecular 557.81
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Fòrmula 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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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)
NB-533 Related Classifications
HY-182429 Related Classifications
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