Lodelaben

Lodelaben is a human neutrophil elastase inhibitor with an IC₅₀ and K_i of 0.5 and 1.5 μM, respectively. IC50 & Target: IC50: 0.5 μM (elastase)^[1]
Ki: 1.5 μM (elastase)^[1] In Vitro: Lodelaben is a human neutrophil elastase inhibitor with an IC₅₀ and K_i of 0.5 and 1.5 μM, respectively. Results indicate that the inhibition of human neutrophil elastase (HNE) by Lodelaben is non-competetive. Lodelaben is not inhibitory at 10 μM with the synthetic substrates or at 5 μM vith Azocoll. Pseudomonas aeruginosa elastase, a metallo-protease is not inhibited by Lodelaben. Cathepsin G activity, however, is inhibited by Lodelaben, with an IC₅₀ of approximately 2.5 μM, with Azocoll as substrate^[1]. In Vivo: The mean pulmonary artery pressures of the saline/vehicle and saline/Lodelaben groups are similar, 16.4±1.1 and 17.4±0.9 mm Hg, respectively. Although, mean pulmonary artery pressure in the monocrotaline/vehicle group is 27.5±0.8 mm Hg, treatment of monocrotaline rats with Lodelaben results in significantly lower values (21.00±1.6 mm Hg, p<0.05). Saline/vehicle and saline/Lodelaben rats have only a small percentage of arteries muscularized at the alveolar wall level (1.9±1.4 and 0.4±0.4%, respectively). Treatment of monocrotaline-injected rats with Lodelaben results in a decreased percentage of alveolar wall arteries muscularized (10.0±3.6%)^[2].