Verubecestat Trifluoroacetate Property

storage temp. 

under inert gas (nitrogen or Argon) at 2-8°C

solubility 

DMSO: 81 mg/mL (154.75 mM);Ethanol: 5 mg/mL (9.55 mM)

Water Solubility 

Water: Insoluble

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Verubecestat Trifluoroacetate Chemical Properties,Usage,Production

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)