MK-8719

Catalog No.S8890 Batch:S889001

Technical Data

Formula	C₉H₁₄F₂N₂O₃S
Molecular Weight	268.28	CAS No.	1382799-40-7
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)
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[2]}	Animal Models rTg4510 mice, Male Sprague-Dawley (SD) rats Dosages 0.1 to 100 mg/kg Administration Oral gavage

Cell Assay:^{^[2]}

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.

Animal Study:^{^[2]}

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

References

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.