Sivelestat sodium tetrahydrate

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.

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.

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.

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