Verubecestat (MK-8931) Trifluoroacetate

Catalog No.S8173 Synonyms: MK-8931

For research use only.

Verubecestat (MK-8931) Trifluoroacetate is a potent and selective beta-secretase inhibitor and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor.

Verubecestat (MK-8931) Trifluoroacetate Chemical Structure

CAS No. 2095432-65-6

Selleck's Verubecestat (MK-8931) Trifluoroacetate has been cited by 10 Publications

Purity & Quality Control

Choose Selective BACE Inhibitors

Biological Activity

Description Verubecestat (MK-8931) Trifluoroacetate is a potent and selective beta-secretase inhibitor and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor.
Targets
BACE2 [1]
(Cell-free assay)
BACE1 [1]
(Cell-free assay)
0.37 nM(Ki) 1.75 nM(Ki)
In vitro

Verubecestat(MK-8931) effectively reduces Aβ40 in cells with a Ki of 7.8 nM and an IC50 of 13 nM[2].

In vivo Verubecestat(MK-8931) dramatically lowers CSF and cortex Aβ40 in both rats and cynomolgus monkeys following a single oral dose. Due to the 20 h half-life of MK-8931 it is ideal for once-a-day dosing[2].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 81 mg/mL
(154.74 mM)
Water Insoluble
Ethanol ''2 mg/mL

Chemical Information

Molecular Weight 523.43
Formula

C19H18F5N5O5S

CAS No. 2095432-65-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1(CS(=O)(=O)N(C(=N1)N)C)C2=C(C=CC(=C2)NC(=O)C3=NC=C(C=C3)F)F.C(=O)(C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02910739 Completed Drug: MK-8931 Amnestic Mild Cognitive Impairment|Alzheimer''s Disease|Prodromal Alzheimer''s Disease Merck Sharp & Dohme Corp. October 11 2016 Phase 1
NCT01537757 Completed Drug: MK-8931 Alzheimer''s Disease Merck Sharp & Dohme Corp. March 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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