1-[[[(1-HYDROXYMETHYL)CYCLOPENTYL]AMINO]ACETYL]-2,5-CIS-PYRROLIDINEDICARBONITRILE HYDROCHLORIDE

General Description

An orally bioavailable dicyanopyrrolidine compound that acts as a slow-binding and active site-targeting inhibitor of DPP IV (IC₅₀ = 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.

Biological Activity

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.