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产品名称：Selleckchem/Alogliptin/S5365

产品编号：S5365

市场价：¥7400.00

场地：美国(厂家直采)

产品分类：其它>耗材>其他>

联系QQ：1570468124

电话号码：4000-520-616

邮箱： info@ebiomall.com

美元价：$370.00

品牌： Selleck Chemicals

公司：Selleckchem

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商品介绍

Description

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.

Targets

DPP-4 ^[1](293E cells lysates)

2.93 nM

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="">^[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].

品牌介绍

Selleck Chemicals提供了超过120,000种用于细胞信号通路研究的抑制剂。我们积极跟踪最新科学，因此我们的客户可以依靠我们成为最新抑制剂的领先供应商。

Selleck的生物活性化合物库由8,000多个具有经过验证的生物学和药理活性的小分子组成。这些分子的安全性和有效性已通过临床前和临床研究证明，其中许多是FDA批准的化合物。

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