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AM-6494 

Cat. No. M28977
AM-6494  Structure
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Biological Activity

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).

Chemical Information
Molecular Weight 473.5
Formula C22H21F2N5O3S
CAS Number 1874232-80-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Samuel C Ugbaja, et al. J Biomol Struct Dyn. Unravelling the molecular basis of AM-6494 high potency at BACE1 in Alzheimer's disease: an integrated dynamic interaction investigation

[2] Samuel C Ugbaja, et al. Biophys Chem. Computational modelling of potent β-secretase (BACE1) inhibitors towards Alzheimer's disease treatment

[3] Michael Frohn, et al. Bioorg Med Chem Lett. The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement

[4] Liping H Pettus, et al. J Med Chem. 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

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  Catalog
Abmole Inhibitor Catalog




Keywords: AM-6494  supplier, Gamma-secretase/Beta-secretase, inhibitors, activators


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