Verubecestat Trifluoroacetate

Biological Activity

Verubecestat (MK-8931) Trifluoroacetat is a potent and selective beta-secretase inhibitor, a BACE1 inhibitor.

in vitro

Verubecestat(MK-8931) effectively reduces Aβ40 in cells, Ki：7.8 nM and IC50 ：13 nM.

in vivo

single oral dose of Verubecestat (MK-8931) to rats and cynomolgus monkeys significantly reduced cerebrospinal fluid (CSF) and cortical Aβ40. MK-8931 has an in vivo half-life of 20 hours, and is suitable for a once-daily dosing frequency.

target

Target	Value
BACE2 (Cell-free assay)	0.37 nM(Ki)
BACE1 (Cell-free assay)	1.75 nM(Ki)