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Art. -Nr.: HY-128774

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AM-6494

AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC₅₀=0.4 nM) with in vivo selectivity over BACE2 (IC₅₀=18.6 nM). AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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CAS. Nr.: 1874232-80-0
Formel: C₂₂H₂₁F₂N₅O₃S
Molecular Weight:473.50

Speicherung:

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

Data Sheet (269 KB)

AM-6494 Chemical Structure

CAS. Nr.: 1874232-80-0

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC₅₀=0.4 nM) with in vivo selectivity over BACE2 (IC₅₀=18.6 nM)^[1]. AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

BACE1

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BACE1
BACE2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	137 μM Compound: 20; AM-6494	Inhibition of recombinant CatD (unknown origin) expressed in CHO cells using FRET peptide substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by FRET assay Inhibition of recombinant CatD (unknown origin) expressed in CHO cells using FRET peptide substrate preincubated for 1 hr followed by substrate addition and measured after 1 hr by FRET assay	[PMID: 31589043]
HEK293	IC₅₀	1.2 nM Compound: 20; AM-6494	Inhibition of BACE in HEK293 cells harboring APP Swedish mutant assessed as reduction in amyloid beta 40 level measured after overnight incubation by sandwich ELISA Inhibition of BACE in HEK293 cells harboring APP Swedish mutant assessed as reduction in amyloid beta 40 level measured after overnight incubation by sandwich ELISA	[PMID: 31589043]
HEK293	IC₅₀	569 nM Compound: 20; AM-6494	Inhibition of recombinant human BACE2 expressed in HEK293 cells co-transfected with N-terminal HA-tagged/C-terminal Myc tagged Mbeta chain of human PMEL17 measured after overnight incubation by Gaussia luciferase reporter gene assay Inhibition of recombinant human BACE2 expressed in HEK293 cells co-transfected with N-terminal HA-tagged/C-terminal Myc tagged Mbeta chain of human PMEL17 measured after overnight incubation by Gaussia luciferase reporter gene assay	[PMID: 31589043]

Chemical Information

CAS. Nr. 1874232-80-0
Molecular Weight 473.50
Formel C₂₂H₂₁F₂N₅O₃S
SMILES

O=C(C1=NC=C(OCC#C)N=C1)NC2=CC(F)=C(F)C([C@@]3(C)N=C(N)S[C@@]4(COC)C[C@@]34[H])=C2
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

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Pettus LH, Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2. J Med Chem. 2019 Oct 18. [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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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

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AM-6494

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