Alogliptin (SYR-322) benzoate

製品コードS2868 バッチS286801

印刷

化学情報

Chemical Structure Synonyms SYR-322 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H21N5O2.C7H6O2
分子量 461.51 CAS No. 850649-62-6
Solubility (25°C)* 体外 DMSO 68 mg/mL (147.34 mM)
Water 2 mg/mL (4.33 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
0.5% methylcellulose
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. 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 Alogliptin (SYR-322) benzoate is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9.
in vitro Alogliptin(SYR-322) is a potent inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. Alogliptin is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30 μM. [1]
in vivo Alogliptin(SYR-322) produces dose-dependent improvements in glucose tolerance and increases plasma insulin levels in female Wistar fatty rats. [1] Acute administration of alogliptin results in a significant decrease in plasma DPP-4 activity, and increases plasma active GLP-1. Alogliptin improves glucose tolerance at a dose of 0.3 mg/kg and higher, with a dose-dependent increase in plasma IRI, suggesting that improved glucose tolerance results from the ability of alogliptin to enhance insulin secretion. [2]

プロトコル(参考用のみ)

キナーゼアッセイ DPP-4 Assay
Solutions of test compounds in varying concentrations (≤10 mM final concentration) are prepared in DMSO and then diluted into assay buffer comprising: 20 mM Tris, pH 7.4; 20 mM KCl and 0.1 mg/mL BSA. Human DPP-4 (0.1 nM final concentration) is added to the dilutions and pre-incubats for 10 minutes at ambient temperature before the reaction is initiated with A-P-7-amido-4-trifluoromethylcoumarin (AP-AFC; 10 μM final concentration). The total volume of the reaction mixture is 10-100 μL depending on assay formats used (384 or 96 well plates). The reaction is followed kinetically (excitation λ= 400 nm; emission λ= 505 nm) for 5 - 10 minutes or an end-point is measured after 10 minutes. Inhibition constants (IC50) are calculated from the enzyme progress curves using standard mathematical models.
動物実験 動物モデル The N-STZ-1.5 rats
投薬量 0.1, 0.3, 1 or 3 mg/kg
投与方法 p.o.

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：

The Tumor Suppressor p53 Limits Ferroptosis by Blocking DPP4 Activity [ Cell Rep, 2017, 20(7):1692-1704] PubMed: 28813679

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。