Alogliptin BenzOATe 是一种有效且特异性的 DPP-4 抑制剂 ,IC50值小于 10 nM,其选择性比 DPP-8/9 高 10,000 倍以上,可用于研究 2 型糖尿病。
产品描述
Alogliptin Benzoate(SYR 322), an effective and specific DPP-4 inhibitor (IC50<10 nM), exhibits greater than 10, 000-fold selectivity over DPP-8/9. Alogliptin may inhibit inflammatory responses by preventing the toll-like receptor 4 (TLR-4)-mediated formation of proinflammatory cytokines.
体外活性
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]
体内活性
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]
Cas No.
850649-62-6
分子式
C25H27N5O4
分子量
461.522
别名
SYR 322;Alogliptin(SYR-322)benzoate;苯甲酸阿格列汀
储存和溶解度
DMSO:63 mg/mL (136.5 mM)
Ethanol:<1 mgml
H2O:2 mg/mL (4.33 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years