L-680833

L-680833 is a monocyclic β-lactam inhibitor of human polymorphonuclear leukocyte elastase (PMNE) inhibitor. L-680833 can be used for the study of PMNE-damaged tissue diseases^[1]. In Vitro:L-680833 inhibits generation of the specific N-terminal cleavage product A alpha-(1-21) from the A alpha chain of fibrinogen by enzyme released from isolated polymorphonuclear leukocytes stimulated with fMet-Leu-Phe with an IC₅₀ of 0.06 μM^[1]. In Vivo:Pharmacokinetic studies indicate that after oral dosing L-680833 is bioavailable in rats and rhesus monkeys. This oral bioavailability is reflected by the inhibition (i) of tissue damage elicited in hamster lungs by intratracheal instillation of human PMNE and (ii) enzyme released from human PMN stimulated after their transfer into the pleural cavity of mice^[1].