Sivelestat sodium tetrahydrate

Catalog No.S4666 Batch:S466604

Technical Data

Formula

C₂₀H₂₁N₂O₇S.4H₂O.Na

Molecular Weight

528.51

CAS No.

201677-61-4

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (189.21 mM)

Ethanol

5 mg/mL (9.46 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 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 500 μL of 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	0.83mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 16.6 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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Sivelestat sodium tetrahydrate (ONO5046-Na, EI546, LY544349) is a competitive inhibitor of human neutrophil elastase, also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse.

Targets

neutrophil elastase ^[1]

In vitro

Sivelestat suppresses both adhesion and transmigration of neutrophils to the endothelium^[2].

In vivo

Intraoperative administration of sivelestat effectively reduced neutrophil induction and activation in the lung and improved oxygenation after cardiopulmonary bypass in a piglet model^[1].By inhibiting neutrophil elastase, sivelestat has a direct action to the accumulated and activated leucocytes, offering efficient protection against the production of oxygen radicals and cytokines^[3].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines human umbilical vein endothelial cell (HUVEC) Concentrations 1, 10, and 50 μg/mL Incubation Time 1 h Method HUVEC are grown to confluence on fibronectin (25 μg/mL) coated Falcon cell culture inserts. Neutrophils stimulated by PAF (0.1 mM) are added to the HUVEC monolayers (upper chamber). The upper chamber is exposed to 2 mL of HUMEDIA and rehydrated at 37 ℃ for 1 h in the absence or the presence (50 μg/mL) of sivelestat. Subsequently, the upper chamber is removed and the fluid in the lower chamber is collected.
Animal Study:^{^[1]}	Animal Models Neonatal piglets Dosages 2 mg/kg/h Administration Intraoperative administration

Cell Assay:^{^[2]}

Cell lines
human umbilical vein endothelial cell (HUVEC)
Concentrations
1, 10, and 50 μg/mL
Incubation Time
1 h
Method
HUVEC are grown to confluence on fibronectin (25 μg/mL) coated Falcon cell culture inserts. Neutrophils stimulated by PAF (0.1 mM) are added to the HUVEC monolayers (upper chamber). The upper chamber is exposed to 2 mL of HUMEDIA and rehydrated at 37 ℃ for 1 h in the absence or the presence (50 μg/mL) of sivelestat. Subsequently, the upper chamber is removed and the fluid in the lower chamber is collected.

Animal Study:^{^[1]}

Animal Models
Neonatal piglets
Dosages
2 mg/kg/h
Administration
Intraoperative administration

References

Selleck's Sivelestat sodium tetrahydrate has been cited by 5 publications

Inhibition of Efferocytosis by Extracellular CIRP-Induced Neutrophil Extracellular Traps [ J Immunol, 2021, 206(4):797-806]	PubMed: 33380498
Neutrophil extracellular traps amplify neutrophil recruitment and inflammation in neutrophilic asthma by stimulating the airway epithelial cells to activate the TLR4/ NF-κB pathway and secrete chemokines [ Aging (Albany NY), 2020, 12(17):16820-16836]	PubMed: 32756014
Identification of Small-Molecule Inhibitors of Brucella Diaminopimelate Decarboxylase by Using a High-Throughput Screening Assay. [ Front Microbiol, 2020, 10:2936]	PubMed: 32038511
Inhibition of Efferocytosis by Extracellular CIRP-Induced Neutrophil Extracellular Traps [ J Immunol, 2020, ji2000091]	PubMed: 33380498
Inhibitors of elastase stimulate murine B lymphocyte differentiation into IgG- and IgA-producing cells [ Eur J Immunol, 2018, 48(8):1295-1301]	PubMed: 29710424

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.