Alogliptin,850649-61-5

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YZ剂描述：

产品名称：Alogliptin

产品别名：阿格列汀

英文别名：SYR-322

靶点：DPP-4

CAS：850649-61-5

纯度：>98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Alogliptin是一种有效的，选择性的DPP-4YZ剂，IC50为<10 nM，比作用于DPP-8和DPP-9选择性高10000倍以上。Alogliptin(SYR-322)是一种强有效的DPP-4YZ剂，比其它非常相近的丝氨酸蛋白酶DPP-8和DPP-9的选择性高出10,000倍。Alogliptin 不会YZCYP-450 酶活性并且直到30μM浓度也不会阻断hERG 通道。

溶解性：DMSO ：68 mg/mL (200.35 mM)
Water ：2 mg/mL (5.89 mM)

体外研究：

Alogliptin is a potent (IC50 .Compound 10 is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30μM.

体内研究：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 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..

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