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Sivelestat

Name: Sivelestat
Brand: Selleck Chemicals
SKU: S8136
Rating: 5 (14 reviews)

Synonyms: ONO-5046, LY544349, EI546

Catalog No.S8136 Purity:99.32%

Sivelestat is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. It almost shows no activity at a range of other proteases.

Sivelestat Chemical Structure

CAS No. 127373-66-4

Purity & Quality Control

Batch: Purity: 99.32%

99.32

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Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Protease Inhibitor Library Ubiquitination Compound Library	Click to Expand

Cell Data

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

Biological Activity

Description

Sivelestat is a potent and selective inhibitor of neutrophil elastase with IC50 of 44nM. It almost shows no activity at a range of other proteases.

Targets

neutrophil elastase ^[1]

In vitro
In vitro	sivelestat reduces the levels of inflammatory mediators by inhibiting NF-kB^[3]. It suppresses the growth of gastric cancer cells by inhibiting the release of TGF-α stimulated by NE^[2]; Sivelestat suppresses iNOS gene expression in proinflammatory cytokine-stimulated hepatocytes^[4].
Cell Research	Cell lines	TMK-1 gastric carcinoma cells
	Concentrations	0.1–1000 µg/mL
	Incubation Time	24, 48 or 72 h
	Method	Gastric carcinoma cells are seeded into 96-well culture plates (5 × 10³ cells/well) in RPMI containing 7% FBS, 2.0 mM L-glutamine, and 1% nonessential amino acids. Following 24-h incubation in RPMI-1640 medium with 5% FBS, the cells are incubated for 24, 48 or 72 h at 37°C in a humidified atmosphere of 5% CO2 with varied concentrations (0.1–1.0 µg/mL) of NE, or with varied concentrations (0.1–1000 µg/mL) of sivelestat or with concentrations (10 and 100 ng/mL) of anti-TGF-α antibody in the presence of 1 µg/mL NE. After incubation, 10 µL of MTT solution (5 mg/mL) is added to each well and the plates are then incubated for 3 h at 37°C. The growth medium is then replaced with 150 µL of dimethyl sulfoxide (Wako) per well and the absorbance at 540 nm is measured using a Titertek Multiscan (Titertek, Huntsville, AL).

In Vivo
In vivo	sivelestat could attenuate sepsis-related kidney injury in rats^[1]. It blocks GAPDH/Siah1 which is a novel signaling pathway during the progression of spinal cord injury^[5]. Administration of sivelestat attenuates pulmonary fibrosis after acute lung injury in mice.
Animal Research	Animal Models	Male Sprague-Dawley rats
	Dosages	50 or 100 mg/kg
	Administration	i.p.

References

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Chemical Information & Solubility

Molecular Weight	434.46	Formula	C₂₀H₂₂N₂O₇S
CAS No.	127373-66-4	SDF	Download Sivelestat SDF
Smiles	CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 87 mg/mL ( (200.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 8 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5% DMSO 1 95% corn oil	1.0mg/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.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.25mg/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 Corn oil	1.86mg/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.
Clear solution	2% DMSO 1 40% PEG 300 2 5%Tween80 3 53%ddH2O	3.6mg/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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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