Sivelestat

Synonyms: ONO-5046, LY544349, EI546

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

Sivelestat Chemical Structure

CAS: 127373-66-4

Selleck's Sivelestat has been cited by 13 publications

Purity & Quality Control

Batch: Purity: 99.32%
99.32

Sivelestat Related Products

Choose Selective Serine Protease Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation 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.

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)

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

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Sivelestat | Sivelestat supplier | purchase Sivelestat | Sivelestat cost | Sivelestat manufacturer | order Sivelestat | Sivelestat distributor