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SML4226

MK-8719

Name: MK-8719
Brand: SIGMA

≥98% (HPLC), powder, O-GlcNAcase inhibitor

别名:

(3aR,5S,6S,7R,7aR)-5-(Difluoromethyl)-2-(ethylamino)-5,6,7,7a-tetrahydro-3aH-pyrano[3,2-d]thiazole-6,7-diol, MK 8719, MK8719

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关于此项目

经验公式（希尔记法）:

C₉H₁₄F₂N₂O₃S

化学文摘社编号:

1382799-40-7

分子量:

268.28

NACRES:

NA.21

Assay:

≥98% (HPLC)

Form:

powder

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属性

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

说明

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).

pictograms

GHS07

signalword

Warning

hcodes

H302

pcodes

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

存储类别

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c