MK-8719

製品コードS8890 バッチS889002

印刷

化学情報

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)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.350mg/ml (5.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 27 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.350mg/ml (5.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 27 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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は、hOGAに対して7.9nMのKi値を持つ、O-GlcNAcase (OGA)酵素の選択的かつ強力な低分子阻害剤です。
in vitro	In vitro, this compound is a potent inhibitor of the human OGA enzyme with comparable activity against the corresponding enzymes from mouse, rat, and dog.
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 this compound in the brains of rats and rTg4510 mice. In the rTg4510 mouse model of human tauopathy, this chemical 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.

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

参考

https://pubmed.ncbi.nlm.nih.gov/31487175/
https://pubmed.ncbi.nlm.nih.gov/32493725/

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。