Verubecestat (TFA)

Verubecestat (MK-8931) TFA is an orally active, high-affinity BACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease[1][2].

Product Specifications

CAS Number

[2095432-65-6]

Product Name Alternative

MK-8931 (TFA)

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

Beta-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/verubecestat-tfa.html

Purity

98.32

Solubility

DMSO : 35 mg/mL (ultrasonic; warming)

Smiles

O=C(C1=NC=C(C=C1)F)NC2=CC=C(C([C@@](C)(N=C(N3C)N)CS3(=O)=O)=C2)F.O=C(C(F)(F)F)O

Molecular Formula

C19H18F5N5O5S

Molecular Weight

523.43

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P362+P364-P405-P501

References & Citations

[1]Yan R, et al. Stepping closer to treating Alzheimer's disease patients with BACE1 inhibitor drugs. Transl Neurodegener. 2016 Jul 14;5:13.|[2]Scott JD, et al. Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931) -A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer'sDisease. Med Chem. 2016 Dec 8;59 (23) :10435-10450.