Sivelestat (Synonyms: EI546; LY544349; ONO5046)

Name: Sivelestat
Brand: MedChemExpress
SKU: HY-17443
Rating: 5.0 (30 reviews)

Cat. No.: HY-17443 Purity: 99.68%: Data Sheet
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Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC₅₀ of 44 nM and a K_i 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.

CAS No. : 127373-66-4

Size	Stock	Quantity

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 30 publication(s) in Google Scholar

Other Forms of Sivelestat:

30 Publications Citing Use of MCE Sivelestat

Flow Cytometry

In Vivo Efficacy Study

In Vivo Imaging

: Sivelestat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]; To evaluate this specific effect of NETosis in the Brd7-deficient context, we treated the mice injected with Brd7-KO cells with either Sivelestat (50 mg/kg) or DMSO starting at the 2-week timepoint, which marks the onset of lung metastatic outgrowth. FACS analysis of dissociated lungs isolated at the 4-week timepoint demonstrated a significant decrease in CTLA4 + CD8 + and PD1 + CD8 + T cells upon Sivelestat treatment.

: Sivelestat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]; To evaluate this specific effect of NETosis in the Brd7-deficient context, we treated the mice injected with Brd7-KO cells with either Sivelestat (50 mg/kg) or DMSO starting at the 2-week timepoint, which marks the onset of lung metastatic outgrowth.

: Sivelestat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]; The mice injected with the 4T07-TGL-Brd7 KO cells (Day 0) were i.p. injected with Sivelestat (50 mg/kg) or DMSO control on days -5,-3,-1,1 and on every alternate day thereafter until Week 4. Represent bioluminescence images for the indicated murine cohorts at 30 min, 1 week, and 4 weeks post tumor cell injection.

: Sivelestat purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 5;16(1):1378. [Abstract]; The mice injected with the 4T07-TGL-Brd7 KO cells (Day 0) were i.p. injected with Sivelestat (50 mg/kg) or DMSO control on days -5,-3,-1,1 and on every alternate day thereafter until Week 4. Line graph showing the normalized photon flux for the indicated murine cohorts over time.

: Sivelestat purchased from MedChemExpress. Usage Cited in: Exp Mol Med. 2025 Sep;57(9):2067-2082. [Abstract]; Sivelestat treatment selectively modulates innate immune cell populations in lung and spleen. Data on weight change in the untreated group (infected with SARS-CoV-2 only) and the Sivelestat (10 mg/kg/day, 50 μL, intraperitoneally)/2% DMSO saline treatment group.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	IC₅₀	> 100 μM Compound: 1, ONO-5046	Cytotoxicity against human HEK293T cells after 24 hrs by MTT assay Cytotoxicity against human HEK293T cells after 24 hrs by MTT assay	[PMID: 24224573]
NIH3T3	IC₅₀	> 100 μM Compound: 1, ONO-5046	Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 24 hrs by MTT assay	[PMID: 24224573]
Neutrophil	IC₅₀	0.05 μM Compound: Sivelestat	Inhibition of elastase release in fMLF/CB-induced human neutrophils preincubated for 5 mins before fMLF/CB treatment using methoxysuccinyl-Ala-Ala-Pro-Val-p-nitroanilide as substrate by spectrophotometry Inhibition of elastase release in fMLF/CB-induced human neutrophils preincubated for 5 mins before fMLF/CB treatment using methoxysuccinyl-Ala-Ala-Pro-Val-p-nitroanilide as substrate by spectrophotometry	[PMID: 25650311]
Neutrophil	IC₅₀	50 μM Compound: Sivelestat	Inhibition of FMLP/CB-stimulated elastase release in human neutrophils preincubated for 5 mins before FMLP/CB treatment using MeO-Suc-Ala-Ala-Pro-Val-pnitroanilide by spectrophotometry Inhibition of FMLP/CB-stimulated elastase release in human neutrophils preincubated for 5 mins before FMLP/CB treatment using MeO-Suc-Ala-Ala-Pro-Val-pnitroanilide by spectrophotometry	[PMID: 25036668]
Neutrophil	IC₅₀	> 20 μM Compound: Sivelestat	Inhibition of superoxide generation in fMLF/CB-induced human neutrophils preincubated for 5 mins before fMLF/CB treatment by spectrophotometry Inhibition of superoxide generation in fMLF/CB-induced human neutrophils preincubated for 5 mins before fMLF/CB treatment by spectrophotometry	[PMID: 25650311]

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.

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.

Molecular Weight

434.46

Formula

C₂₀H₂₂N₂O₇S

CAS No.

127373-66-4

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
10 mM	0.2302 mL	1.1509 mL	2.3017 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.68%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (248 KB) HNMR (273 KB) RP-HPLC (215 KB) LCMS (99 KB)

Handling Instructions (2659 KB)

References

[1]. Kawabata K, et al. ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20. [Content Brief]

[2]. Yuichiro Toda, et al. A neutrophil elastase inhibitor, sivelestat, ameliorates lung injury after hemorrhagic shock in rats. Int J Mol Med. 2007 Feb;19(2):237-43. [Content Brief]

[3]. Tomoharu Kono, et al. Neutrophil elastase inhibitor, sivelestat sodium hydrate prevents ischemia-reperfusion injury in the rat bladder. Mol Cell Biochem. 2008 Apr;311(1-2):87-92. [Content Brief]

[4]. Adeleh Sahebnasagh, et al. Neutrophil elastase inhibitor (sivelestat) may be a promising therapeutic option for management of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19. J Clin Pharm Ther. 2020 Aug 28. [Content Brief]

Complete Stock Solution Preparation Table

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
Ethanol / DMSO	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

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.

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Sivelestat (Synonyms: EI546; LY544349; ONO5046)

Customer Review

Other Forms of Sivelestat:

Sivelestat Related Antibodies

30 Publications Citing Use of MCE Sivelestat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Sivelestat Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Sivelestat Related Classifications

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