ONO-5046, a novel inhibitor of human neutrophil elastase
K Kawabata, M Suzuki, M Sugitani, K Imaki… - Biochemical and …, 1991 - Elsevier
K Kawabata, M Suzuki, M Sugitani, K Imaki, M Toda, T Miyamoto
Biochemical and biophysical research communications, 1991•ElsevierAbstract ONO-5046, N-[2-[4-(2, 2-Dimethylpropionyloxy) phenylsulfonylamino] benzoyl]
aminoacetic acid, competitively inhibited human neutrophil elastase (IC 50= 0.044 μM, Ki=
0.2 μM). It also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.
However, ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas
kallikrein, chymotrypsin and cathepsin G even at 100μM. In in vivo studies, ONO-5046
suppressed lung hemorrhage in hamster (ID 50= 82 μg/kg) by intratracheal administration …
aminoacetic acid, competitively inhibited human neutrophil elastase (IC 50= 0.044 μM, Ki=
0.2 μM). It also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.
However, ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas
kallikrein, chymotrypsin and cathepsin G even at 100μM. In in vivo studies, ONO-5046
suppressed lung hemorrhage in hamster (ID 50= 82 μg/kg) by intratracheal administration …
Abstract
ONO-5046, N-[2-[4-(2,2-Dimethylpropionyloxy)phenylsulfonylamino]benzoyl] aminoacetic acid, competitively inhibited human neutrophil elastase (IC50=0.044 μM, Ki = 0.2μM). It also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse. However, ONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100μM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 μg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase.
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