SMILES string
O[C@@H]1[C@]2([H])[C@](SC(NCC)=N2)([H])O[C@@H]([C@H]1O)C(F)F
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Application
MK-8719 may be used in enzyme and cell-based assays to analyze its inhibitory effects on O-GlcNAcase activity and to assess its binding kinetics via surface plasmon resonance.
Biochem/physiol Actions
MK-8719 is an orally available, brain-penetrant, potent and selective O-GlcNAcase (OGA) inhibitor (Ki in nM = 7.9/human, 9.7/rat, 12.1/dog, 9.7/mouse) that upregulates O-linked N-acetylglucosamine (O-GlcNAc) levels both in cultures (EC50 = 52.7 nM in rat PC-12 cells) and in vivo (fold increase = 3.2 in brain and 2.2 in PBMC 8h post 10 mg/kg p.o. in rats). Chronic MK-8719 treatment ameliorates brain atrophy in human mutant tau (P301L) expressing rTg4510 mice (100 mg/kg b.i.d. p.o. from 8 to 32 weeks of age).
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Harold G Selnick et al.
Journal of medicinal chemistry, 62(22), 10062-10097 (2019-09-06)
Inhibition of O-GlcNAcase (OGA) has emerged as a promising therapeutic approach to treat tau pathology in neurodegenerative diseases such as Alzheimer's disease and progressive supranuclear palsy. Beginning with carbohydrate-based lead molecules, we pursued an optimization strategy of reducing polar surface
Shinichiro Matsui et al.
Leukemia, 38(5), 1032-1045 (2024-04-13)
TNF receptor associated factor 6 (TRAF6) is an E3 ubiquitin ligase that has been implicated in myeloid malignancies. Although altered TRAF6 expression is observed in human acute myeloid leukemia (AML), its role in the AML pathogenesis remains elusive. In this
Xiaohai Wang et al.
The Journal of pharmacology and experimental therapeutics, 374(2), 252-263 (2020-06-05)
Deposition of hyperphosphorylated and aggregated tau protein in the central nervous system is characteristic of Alzheimer disease and other tauopathies. Tau is subject to O-linked N-acetylglucosamine (O-GlcNAc) modification, and O-GlcNAcylation of tau has been shown to influence tau phosphorylation and
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