Name: Sivelestat (Ono-5046)
Brand: Selleck Chemicals
SKU: S8136
Availability: InStock
Rating: 5 (20 reviews)

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Quality Control

Batch: Purity: 99.32%

99.32

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP
Featured Inhibitors	Y-27632 Dihydrochloride SB431542 CHIR-99021 (Laduviglusib) RMC-7977 RMC-6236 (Daraxonrasib) MRTX1133 MG132 Z-VAD-FMK VT3989 IAG933

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
BEAS2B	Function assay		6 hrs	Inhibition of human neutrophil elastase-induced decrease in mICAM1 level expressed in BEAS2B cells assessed as cytoprotective activity after 6 hrs by Western blotting analysis	23350733
BEAS2B	Function assay		6 hrs	Inhibition of human neutrophil elastase-induced increase in sICAM1 level in culture medium expressed in BEAS2B cells assessed as cytoprotective activity after 6 hrs	23350733
BEAS2B	Function assay	100 uM	12 hrs	Inhibition of human neutrophil elastase-induced desquamation expressed in BEAS2B cells assessed as cytoprotective activity at 100 uM after 12 hrs by trypan blue staining-based bright field microscopic analysis	23350733
BEAS2B	Function assay	100 uM		Inhibition of human neutrophil elastase-induced cell morphological changes expressed in BEAS2B cells assessed as cytoprotective activity at 100 uM incubated 12 to 24 hr by trypan blue staining-based bright field microscopic analysis	23350733
BEAS2B	Function assay		3 hrs	Inhibition of human neutrophil elastase-induced cell morphological changes expressed in BEAS2B cells assessed as cytoprotective activity after 3 hrs by trypan blue staining-based bright field microscopic analysis	23350733
BEAS2B	Function assay	100 uM		Inhibition of human neutrophil elastase-induced antiproliferative activity expressed in BEAS2B cells assessed as cytoprotectivity at 100 uM by MTT assay	23350733
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 87 mg/mL (200.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.250mg/ml (7.48mM)	Taking the 1 mL working solution as an example, add 50 μL 65 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (2.30mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.860mg/ml (4.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 37.1 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2% DMSO 1 40% PEG 300 2 5%Tween80 3 53%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.600mg/ml (8.29mM)	Taking the 1 mL working solution as an example, add 20 μL of 180 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	434.46	Formula	C₂₀H₂₂N₂O₇S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	127373-66-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ONO-5046, LY544349, EI546			SMILES	CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	neutrophil elastase
In vitro	sivelestat reduces the levels of inflammatory mediators by inhibiting NF-kB. It suppresses the growth of gastric cancer cells by inhibiting the release of TGF-α stimulated by NE; Sivelestat suppresses iNOS gene expression in proinflammatory cytokine-stimulated hepatocytes.
In vivo	sivelestat could attenuate sepsis-related kidney injury in rats. It blocks GAPDH/Siah1 which is a novel signaling pathway during the progression of spinal cord injury. Administration of sivelestat attenuates pulmonary fibrosis after acute lung injury in mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/27430552/ [2] http://onlinelibrary.wiley.com/doi/10.1111/j.1349-7006.2006.00278.x/pdf [3] https://pubmed.ncbi.nlm.nih.gov/19169649/ [4] https://pubmed.ncbi.nlm.nih.gov/21221803/ [5] https://pubmed.ncbi.nlm.nih.gov/27256506/ [6] https://pubmed.ncbi.nlm.nih.gov/22148910/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-20)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07214103	NOT_YET_RECRUITING	Septic Shock; Coagulopathy	University Hospital, Strasbourg, France	2027-08-01	PHASE2
NCT07552610	RECRUITING	Acute Ischemic Stroke; Large Vessel Occlusion; Thrombectomy; Neutrophil Extracellular Trap Formation	Xuanwu Hospital, Beijing	2026-06-22
NCT07156656	NOT_YET_RECRUITING	Type A Aortic Dissection; Organ Failure, Multiple	Shanghai Zhongshan Hospital	2025-09-01	PHASE4
NCT06381661	RECRUITING	Sepsis	Assistance Publique - Hôpitaux de Paris	2026-07-09	PHASE2
NCT07738952	NOT_YET_RECRUITING	Neuromyelitis Optica Spectrum Disorder Attack	Kyushu University	2026-08-17	PHASE1; PHASE2
NCT07118930	RECRUITING	Coronary Heart Disease; Coronary Artery Disease; Coronary Arterial Disease (CAD)	Affiliated Hospital of Nantong University	2025-08-01	PHASE2

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Sivelestat (Ono-5046) Neutrophil Elastase Inhibitor

Chemical Structure

Molecular Weight: 434.46