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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- No. CAS: 1874232-80-0
- Fòrmula: C22H21F2N5O3S
- Peso molecular:473.50
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
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BACE1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
137 μM
Compound: 20; AM-6494
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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
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[PMID: 31589043] |
| HEK293 | IC50 |
1.2 nM
Compound: 20; AM-6494
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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
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[PMID: 31589043] |
| HEK293 | IC50 |
569 nM
Compound: 20; AM-6494
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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
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[PMID: 31589043] |
Chemical Information
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No. CAS 1874232-80-0
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Peso molecular 473.50
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Fòrmula C22H21F2N5O3S
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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
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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)
AM-6494 Related Classifications
HY-128774 Related Classifications
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