1-[[[(1-HYDROXYMETHYL)CYCLOPENTYL]AMINO]ACETYL]-2,5-CIS-PYRROLIDINEDICARBONITRILE HYDROCHLORIDE 化学特性,用途語,生産方法
一般的な説明
An orally bioavailable dicyanopyrrolidine compound that acts as a slow-binding and active site-targeting inhibitor of DPP IV (IC
50 = 106 nM using recombinant human DPP IV and 38, 69, 92, and 100 nM in inhibiting DPP IV activity in plasma from rat, human, monkey, and dog, respectively) with little activity against DPP II, DPP III, DPP VIII, DPP IX, FAP, or APP even at concentrations as high as 30 μM. Reported to lower blood DPP IV activity and augment GLP-1 response in dog and mouse
in vivo.
生物活性
Inhibitor of dipeptidyl peptidase IV (DPP-IV) (IC 50 = 104 nM) that displays selectivity over enzymes with DPP-like activity (IC 50 > 30 μ M). Increases plasma GLP-1 levels and improves glucose tolerance in diabetic mice following oral glucose challenge.
1-[[[(1-HYDROXYMETHYL)CYCLOPENTYL]AMINO]ACETYL]-2,5-CIS-PYRROLIDINEDICARBONITRILE HYDROCHLORIDE 上流と下流の製品情報
原材料
準備製品