| CAS NO: | 127373-66-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 434.46 |
|---|---|
| Formula | C20H22N2O7S |
| CAS No. | 127373-66-4 (free acid); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 86 mg/mL (197.9 mM) |
| Water: <1 mg/mL | |
| Ethanol: 86 mg/mL (197.9 mM) | |
| Solubility (In vivo) | 5% DMSO+40% PEG 300+5% Tween 80+ddH2O: 23mg/mL |
| Synonyms | ONO5046, LY544349, EI546; ONO 5046; ONO5046; ONO-5046; LY544349; LY-544349; LY 544349; EI 546 sodium salt hydrate, Elaspol sodium salt hydrate, LY 544349 sodium salt hydrate, Trade name: Elaspol. |
| In Vitro | In vitro activity: Sivelestat suppresses both adhesion and transmigration of neutrophils to the endothelium Kinase Assay: 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. Cell Assay: HUVEC are grown to confluence on fibronectin (25 μg/mL) coated Falcon cell culture inserts. Neutrophils stimulated by PAF (0.1 mM) are added to the HUVEC monolayers (upper chamber). The upper chamber is exposed to 2 mL of HUMEDIA and rehydrated at 37 ℃ for 1 h in the absence or the presence (50 μg/mL) of sivelestat. Subsequently, the upper chamber is removed and the fluid in the lower chamber is collected. |
|---|---|
| In Vivo | Intraoperative administration of sivelestat effectively reduced neutrophil induction and activation in the lung and improved oxygenation after cardiopulmonary bypass in a piglet model.By inhibiting neutrophil elastase, sivelestat has a direct action to the accumulated and activated leucocytes, offering efficient protection against the production of oxygen radicals and cytokines. |
| Animal model | Neonatal piglets |
| Formulation & Dosage | Dissolved in 0.9% saline solution; 2 mg/kg/h; Intraoperative administration |
| References | Interact Cardiovasc Thorac Surg. 2008 Oct;7(5):785-8; Dig Dis Sci. 2014 Apr;59(4):787-94; BJU Int. 2011 Jan;107(2):329-36. |
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