LY2608204

製品コードS2155 バッチS215501

印刷

化学情報

Chemical Structure 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
* <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.

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生物活性

製品説明 LY2608204 activates glucokinase (GK) with EC50 of 42 nM. Phase 2.
in vitro LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM. [1]
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 LY2608204 concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg LY2608204 dose. The in vivo blood brain barrier permeability of LY2608204 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. [1]

プロトコル(参考用のみ)

キナーゼアッセイ Glucokinase assay
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。

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