| CAS NO: | 201677-61-4 |
| 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 |
| 1g | 电议 |
| Molecular Weight (MW) | 528.51 |
|---|---|
| Formula | C20H21N2O7S.4H2O.Na |
| CAS No. | 201677-61-4 (Sivelestat sodium tetrahydrate); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 100 mg/mL |
| Water: N/A | |
| Ethanol: N/A | |
| SMILES | O=C([O-])CNC(C1=CC=CC=C1NS(=O)(C2=CC=C(OC(C(C)(C)C)=O)C=C2)=O)=O.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Na+] |
| Synonyms | Sivelestat sodium tetrahydrate; Sivelestat Sodium Hydrate; Sivelestat sodium, ONO5046-Na, Sodium sivelestat, EI546 sodium, LY544349 sodium; 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. Chemical Name: sodium (2-((4-(pivaloyloxy)phenyl)sulfonamido)benzoyl)glycinate tetrahydrate. |
| 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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