LY2608204

製品コードS2155 バッチS215501

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₈H₃₇N₃O₃S₃

分子量

559.81

CAS No.

1234703-40-2

Solubility (25°C)*

体外

DMSO

112 mg/mL (200.06 mM)

Ethanol

35 mg/mL (62.52 mM)

Water

Insoluble

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.

* <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	LY2608204はグルコキナーゼ (GK) をEC50 42 nMで活性化します。第2相。
in vitro	LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. This compound also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.
in vivo	LY2608204 decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg dose. The in vivo blood brain barrier permeability of this compound results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.

プロトコル(参考用のみ)

キナーゼアッセイ	Glucokinase assay
キナーゼアッセイ	The human islet GK isoform is expressed in E. coli as (His)₆-tagged fusion protein and purified with metal chelate affinity chromatography. After purification the enzyme is stored in aliquots at concentration 0.8 mg/mL in 25 mM sodium phosphate, 150 mM sodium chloride, 100 mM imidazole, 1 mM dithiothreitol, 50% glycerol at −80 °C. The assay is performed in flat bottom 96-well plates in a final incubation volume of 100 μL. The incubation mixture consists of 25 mM HEPES (pH7.4), 50 mM potassiumchloride, 2.5 mM magnesiumchloride, 2 mM dithiothreitol, 4 U/mL glucose-6-phosphate dehydrogenase from Leuconostoc mesenteroides, 5 mM ATP, 1 mM NAD and a set concentration of glucose. LY2608204 is dissolved in DMSO and then added to the reaction mixture giving the final DMSO concentration of 10%. The reaction is initiated by addition of 20 μL GK and runs for 20 min at 37 °C. The amount of formed NADH is measured as an increase in absorbance at 340 nm using a microplate reader. Absorbance values are used for EC50 calculations.
動物実験	動物モデル	Male Wistar rats at a weight of 225-250 g
	投薬量	1, 3, 6, 10, 20 and 30 mg/kg
	投与方法	Orally, rats are given a 2 g/kg oral glucose bolus 2 hours after LY2608204 administration.

カスタマーフィードバック

: Data from [Data independently produced by , , Nat Commun, 2016, 7:11463]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Identification of mangiferin as a potential Glucokinase activator by structure-based virtual ligand screening [Min Q Sci Rep, 2017, 7:44681]	PubMed: 28317897
Generation of stem cell-derived β-cells from patients with type 1 diabetes. [ Nat Commun, 2016, 7:11463]	PubMed: 27163171

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。