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Chemical Structure| 201677-61-4 Chemical Structure| 201677-61-4

Structure of Sivelestat Sodium Tetrahydrate
CAS No.: 201677-61-4

Chemical Structure| 201677-61-4

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Sivelestat sodium is a competitive inhibitor of human neutrophil elastase (IC50 = 44 nM; Ki=200 nM); also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.

Synonyms: ONO5046 sodium tetrahydrate; EI546 sodium tetrahydrate; ONO-5046

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Product Details of Sivelestat Sodium Tetrahydrate

CAS No. :201677-61-4
Formula : C20H29N2NaO11S
M.W : 528.51
SMILES Code : CC(C)(C)C(OC1=CC=C(S(=O)(NC2=CC=CC=C2C(NCC([O-])=O)=O)=O)C=C1)=O.[H]O[H].[H]O[H].[H]O[H].[H]O[H].[Na+]
Synonyms :
ONO5046 sodium tetrahydrate; EI546 sodium tetrahydrate; ONO-5046
MDL No. :MFCD01937969
InChI Key :PLHREJBSQUSUCW-UHFFFAOYSA-M
Pubchem ID :23663985

Safety of Sivelestat Sodium Tetrahydrate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Description
Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM.This compound is under investigation for its potential use in the treatment of acute lung injury/acute respiratory distress syndrome (ALI/ARDS) or disseminated intravascular coagulation (DIC), particularly in the context of COVID-19[1].[2].[3].[4].

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Post-traumatic knee osteoarthritis model Intraperitoneal injection 10 mg/kg/once weekly Once weekly for 4 weeks Sivelestat sodium hydrate significantly inhibited the induction of structural changes and significantly increased the vertical episode count and ipsilateral static weight bearing of the joint in KOA rats (all P<0.01). It also significantly inhibited TNF-α and IL-6 production, serum nitrite levels, iNOS protein expression and HMGB1 secretion, as well as p50/p65 DNA binding activity and NF-κB and p-IκB protein expression in the joints of KOA rats compared with the model group (all P<0.01). PMC5526152
Female Sprague-Dawley rats Moderate compression spinal cord injury model (35 g for 5 min at T10) Intraperitoneal injection 30 mg/kg Twice daily for 14 days To assess the effects of Sivelestat on vascular stabilization and functional recovery after spinal cord injury. Results demonstrated that Sivelestat treatment significantly upregulated ANGPT-1 expression, inhibited ANGPT-2 and NE expression, reduced the production of inflammatory cytokines and chemokines, preserved blood-spinal cord barrier integrity, decreased glial scar formation, and promoted hindlimb locomotor function recovery. Additionally, Sivelestat alleviated neuropathic pain. PMC6080383
C57BL/6 mice Experimental autoimmune encephalomyelitis (EAE) Intraperitoneal injection 0.05 mg and 0.5 mg Once daily for 10 days To evaluate the therapeutic effect of Sivelestat on Th17 and Th1-induced EAE. Results showed that 0.5 mg Sivelestat significantly attenuated the clinical symptoms of Th17 EAE but had no effect on Th1 EAE. PMC3319834
C57BL/6J mice Renal ischemia-reperfusion injury model Intravenous injection 50 mg/kg Single dose, lasting 24 hours To investigate the protective effect of Sivelestat on renal ischemia-reperfusion injury and its mechanism. Results showed that Sivelestat pretreatment significantly reduced renal Neutrophil elastase (NE), serum creatinine, and blood urea nitrogen levels after renal ischemia-reperfusion, decreased histological damage and cell apoptosis in kidneys, and suppressed the activation of TLR4/Myd88/NF-κB signaling pathway. PMC11466837
C57BL/6 mice Bilateral nephrectomy model Intraperitoneal injection 50 mg/kg Every 11 hours until death To investigate the protective effects of Sivelestat on acute lung injury (ALI) induced by acute kidney injury (AKI). Results showed that Sivelestat reduced neutrophil infiltration in the lung, decreased neutrophil elastase (NE) activity in the lung and plasma, and improved inflammatory responses and survival rates. PMC2947264
Rats Acute lung injury model Intravenous injection 10 mg/kg Single dose To evaluate the protective effect of Sivelestat on acute lung injury, results showed that Sivelestat significantly alleviated lung injury PMC11210789

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05672472 Acute Respiratory Distress Syn... More >>drome Less << NOT_YET_RECRUITING 2025-02-10 -
NCT05020210 ARDS|Inflammatory Response UNKNOWN 2023-08-31 Southern medical university Na... More >>nfang hospital, Guangzhou, 510515, China Less <<
NCT05343338 Aortic Dissection|Acute Lung I... More >>njury/Acute Respiratory Distress Syndrome (ARDS) Less << UNKNOWN 2024-12-31 First Affiliated Hospital of X... More >>ian Jiaotong University, Xi'an, Shaanxi, 710061, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.46mL

1.89mL

0.95mL

18.92mL

3.78mL

1.89mL

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