Home Neuronal Signaling BACE inhibitor Verubecestat (MK-8931) Trifluoroacetate For research use only.

Verubecestat (MK-8931) Trifluoroacetate

Synonyms: MK-8931

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

Verubecestat (MK-8931) Trifluoroacetate Chemical Structure

CAS No. 2095432-65-6

Purity & Quality Control

Verubecestat (MK-8931) Trifluoroacetate Related Products

Signaling Pathway

BACE Signaling Pathways

BACE Signaling Pathway

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
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
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02910739 Completed
Amnestic Mild Cognitive Impairment|Alzheimer''s Disease|Prodromal Alzheimer''s Disease
Merck Sharp & Dohme LLC
 October 11 2016 Phase 1
NCT01537757 Completed
Alzheimer''s Disease
Merck Sharp & Dohme LLC
 March 2012 Phase 1

Chemical Information & Solubility

Molecular Weight 523.43 Formula

C19H18F5N5O5S
CAS No. 2095432-65-6 SDF Download Verubecestat (MK-8931) Trifluoroacetate SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (191.04 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

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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