150374-95-1
Sivelestat Sodium
CAS: 150374-95-1
Molecular Formula: C20H21N2NaO7S
150374-95-1 - Names and Identifiers
150374-95-1 - Physico-chemical Properties
| Molecular Formula | C20H21N2NaO7S |
| Molar Mass | 456.44 |
| Melting Point | 104-108 °C(Solv: water (7732-18-5)) |
| Solubility | DMSO |
| Appearance | White to white-like powder |
| Color | White to Off-White |
| Storage Condition | Desiccate at RT |
| In vitro study | 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 IC 50 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 study | Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID 50 = 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID 50 = 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. Animal Model: Male Golden hamsters, weighing 90 to 110 g. Dosage: 0.021-2.1 mg/kg. Administration: Intratracheally five min before HNE injection. Result: Significantly and dosedependently suppressed the lung hemorrhage. Animal Model: Male Sprague-Dawley rats weighing 350-400 g. Dosage: 10 mg/kg. Administration: Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase. Result: Greatly suppressed lung injury, as revealed by the reduced histological damage. Significantly ameliorated HSR-induced lung injury. Markedly decreased the levels of TNF-α and iNOS gene. Animal Model: Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g. Dosage: 15 mg/kg or 60 mg/kg. Administration: IP. Result: Decreased the blood flow in the bladder during reperfusion phase compared to the IR group. |
150374-95-1 - Reference
| Reference Show more | 1. [IF=5.396] Zhu Tao et al."Evaluation of the anti-inflammatory properties of the active constituents in Ginkgo biloba for the treatment of pulmonary diseases."Food Funct. 2019 Apr;10(4):2209-2220 |
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