Alogliptin

製品コードS5365 バッチS536501

印刷

化学情報

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

C18H21N5O2
分子量 339.39 CAS No. 850649-61-5
Solubility (25°C)* 体外 DMSO 67 mg/mL (197.41 mM)
Ethanol 67 mg/mL (197.41 mM)
Water 18 mg/mL (53.03 mM)
* <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 Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4)with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.
in vitro Alogliptin is a potent (IC50 < 10 nM) inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9[1].Compound 10 is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30μM[2].
in vivo Absolute oral bioavailability of alogliptin in rats, dogs, and monkeys is 45%, 86%, and 72% to 88%, respectively. After a single oral dose of alogliptin, plasma DPP-4 inhibition is observed within 15 min and maximum inhibition is > 90% in rats, dogs, and monkeys; inhibition is sustained for 12 h in rats (43%) and dogs (65%) and 24 h in monkeys (> 80%). From Emax modeling, 50% inhibition of DPP-4 activity is observed at a mean alogliptin plasma concentration (EC50) of 3.4 to 5.6 ng/ml (10.0 to 16.5 nM) in rats, dogs, and monkeys. In Zucker fa/fa rats, a single dose of alogliptin (0.3, 1, 3, and 10 mg/kg) inhibites plasma DPP-4 (91% to 100% at 2 h and 20% to 66% at 24 h), increases plasma GLP-1 (2- to 3-fold increase in AUC0–20 min) and increases early-phase insulin secretion (1.5- to 2.6-fold increase in AUC0-20 min) and reduces blood glucose excursion (31%–67% decrease in AUC0–90 min) after oral glucose challenge. Alogliptin (30 and 100 mg/kg) has no effect on fasting plasma glucose in normoglycemic rats.[3].

プロトコル(参考用のみ)

キナーゼアッセイ Evaluate the inhibitory potency of DPP4 inhibitors based on DPP8/9 enzymatic activity assay
hDPP8/9 over-expressing 293E cells are lysed and 100 μg of lysate is added in the enzymatic activity assay. Within 100 μl of the final volume, the final concentration of DPP inhibitors used in the assay is 10 μM, DMSO at the concentration of 0.1% is applied as a solvent and negative control, and the final concentration of Gly-Pro-p-nitroanilide is 0.26 mM. The OD value is detected immediately before and after 40 min of reaction at 37 °C, and then enzymatic activity is calculated.
動物実験 動物モデル db/db mice
投薬量 76.4 mg/kg/day
投与方法 oral

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 SARS-CoV-2-induced pathways reveals drug repurposing strategies [ Sci Adv, 2021, 7(27)eabh3032] PubMed: 34193418

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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