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

Sivelestat  (Synonyms: EI546; LY544349; ONO5046)

Cat. No.: HY-17443 Purity: 98.61%
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Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) 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 Chemical Structure

Sivelestat Chemical Structure

CAS No. : 127373-66-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 92 In-stock
Solution
10 mM * 1 mL in DMSO USD 92 In-stock
Solid
5 mg USD 54 In-stock
10 mg USD 84 In-stock
50 mg USD 288 In-stock
100 mg   Get quote  
200 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

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Based on 17 publication(s) in Google Scholar

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Sivelestat Related Antibodies

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  • Purity & Documentation

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  • Customer Review

Description

Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) 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].

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

Sivelestat Related Antibodies
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].

MedChemExpress (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

434.46

Formula

C20H22N2O7S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(C)C(OC1=CC=C(S(=O)(NC2=CC=CC=C2C(NCC(O)=O)=O)=O)C=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (230.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 3.03 mg/mL (6.97 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3017 mL 11.5085 mL 23.0171 mL
5 mM 0.4603 mL 2.3017 mL 4.6034 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.3017 mL 11.5085 mL 23.0171 mL 57.5427 mL
5 mM 0.4603 mL 2.3017 mL 4.6034 mL 11.5085 mL
DMSO 10 mM 0.2302 mL 1.1509 mL 2.3017 mL 5.7543 mL
15 mM 0.1534 mL 0.7672 mL 1.5345 mL 3.8362 mL
20 mM 0.1151 mL 0.5754 mL 1.1509 mL 2.8771 mL
25 mM 0.0921 mL 0.4603 mL 0.9207 mL 2.3017 mL
30 mM 0.0767 mL 0.3836 mL 0.7672 mL 1.9181 mL
40 mM 0.0575 mL 0.2877 mL 0.5754 mL 1.4386 mL
50 mM 0.0460 mL 0.2302 mL 0.4603 mL 1.1509 mL
60 mM 0.0384 mL 0.1918 mL 0.3836 mL 0.9590 mL
80 mM 0.0288 mL 0.1439 mL 0.2877 mL 0.7193 mL
100 mM 0.0230 mL 0.1151 mL 0.2302 mL 0.5754 mL
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Sivelestat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Sivelestat127373-66-4EI546 LY544349 ONO5046EI 546EI-546LY544349LY 544349LY-544349ONO5046ONO 5046ONO-5046ElastaseSARS-CoVSARS coronavirusAcutelunginjuryischemiareperfusionInhibitorinhibitorinhibit

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