An inhibitor of neutrophil elastase
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Sivelestat (sodium salt hydrate)

Item No. 17779

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,2-dimethyl-propanoic acid, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester, monosodium salt, tetrahydrate
CAS Number
201677-61-4
Synonyms
  • LY544349
  • ONO-5046
Molecular Formula
C20H21N2O7S • Na [4H2O]
Formula Weight
528.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 15 mg/mlEthanol: 0.3 mg/mlPBS (pH 7.2): 2 mg/ml
λmax
210 nm
SMILES
O=S(C1=CC=C(OC(C(C)(C)C)=O)C=C1)(NC2=C(C(NCC([O-])=O)=O)C=CC=C2)=O.[Na+].O.O.O.O
InChi Code
InChI=1S/C20H22N2O7S.Na.4H2O/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24;;;;;/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24);;4*1H2/q;+1;;;;/p-1
InChi Key
PLHREJBSQUSUCW-UHFFFAOYSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    25 mg

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    50 mg

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    Product Description

    Sivelestat is an inhibitor of neutrophil elastase (IC50 = 44 nM for the human enzyme).1 It is selective for neutrophil elastase over trypsin, thrombin, plasmin, kallikrein, chymotrypsin, and cathepsin G at 100 µM. Sivelestat inhibits the formation of neutrophil extracellular traps (NETs) induced by ionomycin (Item Nos. 10004974 | 11932) in isolated mouse neutrophils.2 It decreases LPS-induced NF-κB nuclear translocation in isolated rat pulmonary microvascular endothelial cells (PMVECs) at 50 mM.3 Sivelestat (10 mg/kg) reduces pulmonary edema, increases in the number of cells in the lung tissue positive for myeloperoxidase (MPO), a marker of neutrophil infiltration, and the severity of lung injury in a rat model of LPS-induced acute lung injury.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Basse, L.H., Groen, D., and Bouwstra, J.A. Permeability and lipid organization of a novel psoriasis stratum corneum substitute. Int. J. Pharm. 457(1), 275-282 (2013).

    2. Martinod, K., Witsch, T., Farley, K., et al. Neutrophil elastase-deficient mice form neutrophil extracellular traps in an experimental model of deep vein thrombosis. J. Thromb. Haemost. 14(3), 551-558 (2016).

    3. Yuan, Q., Jiang, Y.-W., and Fang, Q.-H. Improving effect of Sivelestat on lipopolysaccharide-induced lung injury in rats. APMIS 122(9), 810-817 (2014).