产品介绍
Product Description
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).
技术参数
Specifications
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | O[C@@H]1[C@]2([H])[C@](SC(NCC)=N2)([H])O[C@@H]([C@H]1O)C(F)F |
