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MK-8719

Chemical Structure : MK-8719

CAS No.: 1382799-40-7

MK-8719 (MK8719)

货号: PC-72110Not For Human Use, Lab Use Only.

MK-8719 (MK8719) is a a highly potent, selective, CNS-penetrable inhibitor of O-GlcNAcase (OGA) with Ki of 7.9 nM (hOGA).

规格 价格 库存 数量
5 mg ¥1980 In stock
10 mg ¥2980 In stock
25 mg ¥4980 In stock
50 mg Get quote
100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MK-8719 (MK8719) is a a highly potent, selective, CNS-penetrable inhibitor of O-GlcNAcase (OGA) with Ki of 7.9 nM (hOGA).
MK-8719 displays no effect against human hexosaminidase A/B (HexA/B) and human N-acetylglucosaminidase (NAGLU), as well as a panel of > 100 receptor and enzyme targets.
MK-8719 inhibits human OGA enzyme with comparable activity against the corresponding enzymes from mouse, rat, and dog.
MK-8719 produces a dose-dependent increase in O-GlcNAc in PC12 cells with IC50 of 52.7 nM.
MK-8719 elevates brain and peripheral blood mononuclear cell O-GlcNAc levels in a dose-dependent manner in vivo, demonstrateed robust target engagement in the brains of rats and rTg4510 mice.

物理化学性质&存储条件

分子量 268.279
分子式 C9H14F2N2O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(3aR,5S,6S,7R,7aR)-5-(difluoromethyl)-2-(ethylamino)-3a,6,7,7a-tetrahydro-5H-pyrano[3,2-d]thiazole-6,7-diol

参考文献

1. Wang X, et al. J Pharmacol Exp Ther. 2020 Aug;374(2):252-263.

2. Selnick HG, et al. J Med Chem. 2019 Nov 27;62(22):10062-10097.

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