1. Metabolic Enzyme/Protease
    Anti-infection
  2. Elastase
    SARS-CoV
  3. Sivelestat sodium

Sivelestat sodium (Synonyms: ONO5046-Na; Sodium sivelestat; EI546 sodium; LY544349 sodium)

Cat. No.: HY-17443A Purity: 99.13%
Handling Instructions

Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.

For research use only. We do not sell to patients.

Sivelestat sodium Chemical Structure

Sivelestat sodium Chemical Structure

CAS No. : 150374-95-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 93 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 288 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19[1][2][3][4].

In Vitro

Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM[1].
Sivelestat (ONO-5046) exhibits IC50 values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID50 = 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase[1].
Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats[2].
Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Golden hamsters, weighing 90 to 110 g[1].
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[2].
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[3].
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.
Clinical Trial
Molecular Weight

456.44

Formula

C₂₀H₂₁N₂NaO₇S

CAS No.

150374-95-1

SMILES

CC(C)(C)C(OC1=CC=C(S(=O)(NC2=CC=CC=C2C(NCC(O[Na])=O)=O)=O)C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.09 mM; Need ultrasonic)

H2O : 1 mg/mL (2.19 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1909 mL 10.9543 mL 21.9087 mL
5 mM 0.4382 mL 2.1909 mL 4.3817 mL
10 mM 0.2191 mL 1.0954 mL 2.1909 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.13%

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Keywords:

SivelestatONO5046-Na Sodium sivelestatEI546LY544349EI 546EI-546LY 544349LY-544349ElastaseSARS-CoVSARS coronavirusAcutelunginjuryischemiareperfusionInhibitorinhibitorinhibit

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Sivelestat sodium
Cat. No.:
HY-17443A
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