MK-8719

製品コードS8890 バッチS889002

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C9H14F2N2O3S
分子量 268.28 CAS No. 1382799-40-7
Solubility (25°C)* 体外 Ethanol 54 mg/mL (201.28 mM)
DMSO 27 mg/mL (100.64 mM)
Water 14 mg/mL (52.18 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 MK-8719 is a selective and potent small molecule inhibitor of the O-GlcNAcase (OGA) enzyme with ki of 7.9nM for hOGA.
in vitro

In vitro, MK-8719 is a potent inhibitor of the human OGA enzyme with comparable activity against the corresponding enzymes from mouse, rat, and dog.[2]
in vivo

In vivo, oral administration of MK-8719 elevates brain and peripheral blood mononuclear cell O-GlcNAc levels in a dose-dependent manner. In addition, positron emission tomography imaging studies demonstrate robust target engagement of MK-8719 in the brains of rats and rTg4510 mice. In the rTg4510 mouse model of human tauopathy, MK-8719 significantly increases brain O-GlcNAc levels and reduces pathologic tau. The reduction in tau pathology in rTg4510 mice is accompanied by attenuation of brain atrophy, including reduction of forebrain volume loss as revealed by volumetric magnetic resonance imaging analysis.[2]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 PC-12 cells
濃度 up to 1 mM
反応時間 24 h
実験の流れ

Rat PC-12 cells are plated in 96-well plates with approximately 10,000 cells/well. Compounds to be tested (including MK-8719) are dissolved in DMSO, either 2- or 10-mM stock solution, and then diluted with DMSO and water in a two-step process using a Tecan workstation. Cells are treated with diluted compounds for 24 hours to reach a final concentration of inhibitor desired to measure a concentration-dependent response, typically, 10 3-fold dilution steps, starting at 10 mM.
動物実験 動物モデル rTg4510 mice, Male Sprague-Dawley (SD) rats
投薬量 0.1 to 100 mg/kg
投与方法 Oral gavage

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。