MK-8719

For research use only.

Catalog No.S8890

MK-8719 Chemical Structure

CAS No. 1382799-40-7

MK-8719 is a selective and potent small molecule inhibitor of the O-GlcNAcase (OGA) enzyme with ki of 7.9nM for hOGA.

Purity & Quality Control

Choose Selective OGA Inhibitors

Biological Activity

Description MK-8719 is a selective and potent small molecule inhibitor of the O-GlcNAcase (OGA) enzyme with ki of 7.9nM for hOGA.
Targets
hOGA [1]
(Cell-free assay)
7.9nM(Ki)
In vitro

In vitro, MK-8719 is a potent inhibitor of the human OGA enzyme with comparable activity against the corresponding enzymes from mouse, rat, and dog.[2]

In vivo

In vivo, oral administration of MK-8719 elevates brain and peripheral blood mononuclear cell O-GlcNAc levels in a dose-dependent manner. In addition, positron emission tomography imaging studies demonstrate robust target engagement of MK-8719 in the brains of rats and rTg4510 mice. In the rTg4510 mouse model of human tauopathy, MK-8719 significantly increases brain O-GlcNAc levels and reduces pathologic tau. The reduction in tau pathology in rTg4510 mice is accompanied by attenuation of brain atrophy, including reduction of forebrain volume loss as revealed by volumetric magnetic resonance imaging analysis.[2]

Protocol

Cell Research:

[2]

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  • Cell lines: PC-12 cells
  • Concentrations: up to 1 mM
  • Incubation Time: 24 h
  • Method:

    Rat PC-12 cells are plated in 96-well plates with approximately 10,000 cells/well. Compounds to be tested (including MK-8719) are dissolved in DMSO, either 2- or 10-mM stock solution, and then diluted with DMSO and water in a two-step process using a Tecan workstation. Cells are treated with diluted compounds for 24 hours to reach a final concentration of inhibitor desired to measure a concentration-dependent response, typically, 10 3-fold dilution steps, starting at 10 mM.


    (Only for Reference)
Animal Research:

[2]

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  • Animal Models: rTg4510 mice, Male Sprague-Dawley (SD) rats
  • Dosages: 0.1 to 100 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 54 mg/mL (201.28 mM)
Water 54 mg/mL (201.28 mM)
Ethanol 54 mg/mL (201.28 mM)

* 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 268.28
Formula

C9H14F2N2O3S

CAS No. 1382799-40-7
Storage powder
in solvent
Synonyms N/A
Smiles CCN=C1NC2C(C(C(OC2S1)C(F)F)O)O

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 ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

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 SDS / 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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    C2
    V2

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

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
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    C4=C3/X C4: LOG(C4):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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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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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID