Mizagliflozin (KWA 0711)

製品コードS8939 バッチS893901

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₈H₄₄N₄O₈

分子量

564.67

CAS No.

666843-10-3

Solubility (25°C)*

体外

DMSO

100 mg/mL (177.09 mM)

Water

100 mg/mL (177.09 mM)

Ethanol

100 mg/mL (177.09 mM)

体内（毎回新しく調製した物を用意してください）

Clear solution	5% DMSO 1 95% Corn oil	0.83mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 16.6 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 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.

* <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	Mizagliflozin (KWA 0711) is a novel, potent, selective sodium glucose co-transporter 1 (SGLT1) inhibitor with Ki of 27 nM for human SGLT1. The selectivity ratio (Ki value for human SGLT2/Ki value for human SGLT1) of mizagliflozin is 303. Mizagliflozin shows the potential use for the amelioration of chronic constipation.
in vitro	Mizagliflozin's inhibitory activity against SGLTs is evaluated by an in vitro assay of cells transiently expressing SGLTs. Mizagliflozin potently inhibits human SGLT1 in a highly selective manner.^[1].
in vivo	The oral administration of Mizagliflozin increased fecal wet weight in a dog model of loperamide-induced constipation and a rat model of low-fiber-diet-induced constipation.^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	COS-7 cells
	濃度	0-1 μM, 0-30 μM
	反応時間	1 h
	実験の流れ	COS-7 cells are transiently transfected with a plasmid expressing human SGLT1 or SGLT2 by using Lipofectamine 2000. Two days after the transfection, the cells are incubated in an uptake buffer containing Mizagliflozin and 14C-labeled AMG at 37 ℃ for 1 h. The cells are then washed and their radioactivity is measured using Topcount. In this experiment, concentrations of 0.3 mM AMG and 1 mM AMG in the uptake buffer are used to calculate Ki values.
動物実験	動物モデル	Male Wistar rats, male Beagle dogs
	投薬量	2 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg, 80 mg/kg, 160 mg/kg
	投与方法	Oral gavage

参考

[1] Inoue T, et al. Eur J Pharmacol. 2017 Jul 5;806:25-31.

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。