Lodelaben is a human neutrophilelastaseinhibitor with anIC₅₀andK_iof 0.5 and 1.5 μM, respectively.

IC50: 0.5 μM (elastase)^[1]
Ki: 1.5 μM (elastase)^[1]

Lodelaben is a human neutrophil elastase inhibitor with an IC₅₀and K_iof 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 IC₅₀of approximately 2.5 μM, with Azocoll as substrate^[1].

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].

425.04

Solid

C₂₅H₄₁ClO₃

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氯德拉苯

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