Lodelaben (Declaben, SC-39026) is a reversible, non-competitive inhibitor of human neutrophil elastase (HNE), characterized by specificity and potency (IC50=0.5 μM, Ki=1.5 μM).

Elastase:0.5 μM, Elastase:1.5 μM (Ki)

Lodelaben is a human neutrophil elastase inhibitor with IC50 and Ki50 of 0.5 and 1.5 μM, respectively. Lodelaben can inhibit human neutrophil elastase (HNE) in a non-competitive manner. [1]

Methods: Lodelaben (SC-39026) (40 mg/kg, gavage, 8 days) was administered to male Sprague-Dawley rats 8 days after a single subcutaneous injection of monocrotaline (60 mg/kg) or saline. Thirteen days after injection, an indwelling cardiovascular catheter was inserted under pentobarbital anesthesia, and 15 days after injection, pulmonary and systemic hemodynamic measurements were recorded while the animals were awake, and at necropsy, the lungs were perfused and evaluated by light and electron microscopy using morphometric techniques.
Results: Saline-injected rats given Lodelaben or vehicle were similar in all characteristics evaluated. In contrast, mean pulmonary artery pressure was significantly lower in monocrotaline rats injected with SC-39026 than in rats given vehicle (21.0 +/- 1.6 vs. 27.5 +/- 0.8 mm Hg, p less than 0.05), which was associated with a significant reduction in the number of muscularized arteries at the alveolar wall level (r2 = 0.89, p less than 0.001).[3]