Verubecestat (MK-8931)

For research use only.

Catalog No.S8564

2 publications

Verubecestat (MK-8931) Chemical Structure

CAS No. 1286770-55-5

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

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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

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

Solubility (25°C)

In vitro DMSO 81 mg/mL (197.84 mM)
Ethanol 41 mg/mL (100.14 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 409.41
Formula

C17H17F2N5O3S

CAS No. 1286770-55-5
Storage powder
in solvent
Synonyms N/A
Smiles CC1(CS(=O)(=O)N(C(=N1)N)C)C2=C(C=CC(=C2)NC(=O)C3=NC=C(C=C3)F)F

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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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

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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BACE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID