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Verubecestat (MK-8931)

Name: Verubecestat (MK-8931)
Brand: Selleck Chemicals
SKU: S8564
Rating: 5 (6 reviews)

Catalog No.S8564 Purity:99.68%

Verubecestat (MK-8931) is a potent and selective beta-secretase (also known as Beta-site APP-cleaving enzyme 1) inhibitor.

Verubecestat (MK-8931) Chemical Structure

CAS No. 1286770-55-5

Purity & Quality Control

Batch: Purity: 99.68%

99.68

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Signaling Pathway

BACE Signaling Pathway

Biological Activity

Description

Verubecestat (MK-8931) is a potent and selective beta-secretase (also known as 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

Chemical Information & Solubility

Molecular Weight	409.41	Formula	C₁₇H₁₇F₂N₅O₃S
CAS No.	1286770-55-5	SDF	Download Verubecestat (MK-8931) 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
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 82 mg/mL ( (200.28 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 11 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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

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