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Cat. No.: 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 No.: 1874232-80-0
Formule: C₂₂H₂₁F₂N₅O₃S
Masse moléculaire:473.50

Stockage:

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

Data Sheet (269 KB)

AM-6494 Chemical Structure

CAS No.: 1874232-80-0

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Use of MCE Products

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

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

Voir tous les produits spécifiques à Isoform Beta-secretase :

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 No. 1874232-80-0
Masse moléculaire 473.50
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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

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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

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
Chemical Information
Pureté et documentation
Références

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AM-6494

Voir tous les produits spécifiques à Isoform Beta-secretase