DESCRIPTION MK-8719 is a highly potent and selective O-GlcNAcase (OGA) inhibitor (Ki=7.9 nM for hOGA) with excellent CNS penetration[1].

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DESCRIPTION MK-8719 is an inhibitor of O-GlcNAcase (OGA) that is being investigated as a disease modifying strategy for neurodegenerative tauopathies (including Alzheimer's disease, Pick's disease and progressive supranuclear palsy) . Development of MK-8719 is the result of a partnership between Merck and Alectos Therapeutics. MK-8719 was designed using on the scaffold of the carbohydrate-based lead molecule and used medicinal chemistry and SAR to improve on thiamet-G's less than favourable drug-like properties (e.g. potency, selectivity, CNS exposure and metabolic stability). The current status of OGA inhibitor development as a novel preventative mechanism in neurodegeneration and age-related memory impairment is reveiwed by Rudrawar and Ryan (2019) . (GtoPdb)

DESCRIPTION MK-8719 is a highly potent and selective inhibitor of O-GlcNAcase (OGA) [hOGA], with a Ki value of 7.9 nM. (TargetMol Bioactive Compound Library)