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MK-8719

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

MK-8719 Chemical Structure

MK-8719 Chemical Structure

CAS: 1382799-40-7

Purity & Quality Control

Batch: Purity: 99.61%
99.61

MK-8719 Related Products

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

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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models rTg4510 mice, Male Sprague-Dawley (SD) rats
Dosages 0.1 to 100 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 268.28 Formula

C9H14F2N2O3S
CAS No. 1382799-40-7 SDF --
Smiles CCN=C1NC2C(C(C(OC2S1)C(F)F)O)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 54 mg/mL ( (201.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 54 mg/mL

Ethanol : 54 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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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 %

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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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