Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE)[1][2].
Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/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 [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2].
Ala-Ala-Pro-Val-chloromethylketone is an irreversible human neutrophil elastase (NE) inhibitor for use in the study of chronic inflammatory airway diseases[1].
Aristololactam IIIa exhibits significant inhibitory effects on superoxide anion generation and elastase release with IC50 values of 0.12 and 0.20 μg/mL, respectively[1].
Elastase-IN-1 (Compound Q11) is an elastase inhibitor with an IC50 of 0.897 µM. Elastase-IN-1 is non-toxic[1].
Suc-Ala-Ala-Ala-AMC is a peptide substrate of elastase or elastase-like[1].
MeOSuc-Ala-Ala-Pro-Met-AMC is a peptide substrate of elastases and chymotrypsin-like serine peptidases[1].
Suc-Ala-Ala-Pro-Val-AMC, a tetrapeptide, is an elastasesubstrate. Suc-Ala-Ala-Pro-Val-AMC can be used for determining elastase activity[1][2].
AE-3763 is a peptide-based human neutrophil elastase inhibitor with an IC50 of 29 nM.