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Art. -Nr.: HY-182429

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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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CAS. Nr.: 1146544-18-4
Formel: C₃₃H₅₅N₃O₄
Molecular Weight:557.81

Speicherung:

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

NB-533 Chemical Structure

CAS. Nr.: 1146544-18-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

BACE1

0.002 μM (IC₅₀)

Cathepsin D

0.001 μM (IC₅₀)

Alle Beta-secretase Isoform-spezifische Produkte anzeigen :

BACE1
BACE2

Alle Cathepsin Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	24 μM Compound: 14, NB-533	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	[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.

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.

Chemical Information

CAS. Nr. 1146544-18-4
Molecular Weight 557.81
Formel C₃₃H₅₅N₃O₄
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Machauer R, et al. Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo. Bioorg Med Chem Lett. 2009;19(5):1366-1370. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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NB-533

Alle Beta-secretase Isoform-spezifische Produkte anzeigen

Alle Cathepsin Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

NB-533 Related Classifications

HY-182429 Related Classifications