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Antiviral API
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Sivelestat
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| Category | SARS-CoV |
| CAS | 127373-66-4 |
| Description | Sivelestat is a competitive human neutrophil elastase (HNE) inhibitor (IC50 = 44 nM, Ki = 0.2 μM). It also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse (IC50 = 19 to 49 nM). However, it does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM. In in-vivo studies, it 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. |
Product Information
| Synonyms | EI546; EI 546; EI-546; LY544349; LY 544349; LY-544349; ONO5046; ONO-5046; ONO 5046 |
| Molecular Weight | 434.46 |
| Molecular Formula | C20H22N2O7S |
| Canonical SMILES | CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O |
| Purity | >98% |
| Density | 1.4±0.1 g/cm3 |
| Solubility | In vitro: 10 mM in DMSO |
| Appearance | White to off-white (Solid) |
| Storage | 4°C, protect from light * In solvent : -80°C, 6 months -20°C, 1 month (protect from light) |
| Complexity | 731 |
| Exact Mass | 434.11477222 |
| Index Of Refraction | 1.598 |
| In Vitro | Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM. Sivelestat (ONO-5046) exhibits IC50 values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively, |
| In Vivo | Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID50 = 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats Sivelestat (15, 60 mg/kg, ip) prevents ischemia-reperfusion injury in the rat bladder. |
| PSA | 147.25000 |
| Target | Elastase; SARS-CoV |
| XLogP3-AA | 3 |
