SivelestatAn inhibitor of elastase

Sivelestat (CAS 127373-66-4)

Sivelestat | CAS 127373-66-4 is rated 5.0 out of 5 by 1.
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Synonym: Elastase Inhibitor IV
Application: An inhibitor of elastase
CAS Number: 127373-66-4
Purity: ≥95%
Molecular Weight: 434.46
Molecular Formula: C20H22N2O7S
* Refer to Certificate of Analysis for lot specific data (including water content).
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Sivelestat is a cell-permeable sulfanilide compound that acts as a potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC50 = 19-49 nM in rat, rabbit, hamster, human, and mouse leukocyte elastase). Sivelestat displays >100-fold greater selectivity over pancreas elastase (IC50 = 5.6 μM). Sivelestat does not inhibit trypsin, thrombin, plasmin, kallikrein, chymotrypsin, and cathepsin G even at concentrations as high as 100 μM. Sivelestat effectively suppresses human neutrophil elastase-induced lung hemorrhage and skin capillary permeability. Sivelestat is also reported to inhibit mast cell Stat6-protease.


References

1. Suzuki, K., et al. 2003. Biochem. Biophys. Res. Commun. 309, 768. 2. Kawabata, K., et al. 1991. Biochem. Biophys. Res. Commun. 177, 814.

Physical State :
Solid
Solubility :
Soluble in DMSO.
Storage :
Store at 4° C
Melting Point :
218-220° C
Density :
1.37 g/cm3 (Predicted)
Refractive Index :
n20D 1.60 (Predicted)
IC50 :
Neutrophil Elastase: IC50 = 44 nM (human)
Ki Data :
Neutrophil Elastase: Ki= 200 nM (human)
pK Values :
pKa: 3.67 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
107706
MDL Number :
MFCD00889071
SMILES :
CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O

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Certificate of Analysis

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Sivelestat  Product Citations

See how others have used Sivelestat. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 23155475  Gill, N. et al. 2012. PLoS ONE. 7: e49646.

Citations 1 to 1 of 1 total

I also want to know if this neutrophile elastase inhibitor could inhibit Pseudomonas elastase? I wonder if your campany have some information or products to specifically inhibit Pseudomonas elastase? Otherwise can you customize product?

Asked by: Jian L
Thank you for your question. In the context of this chemical, Sivelestat, there doesn’t seem to be any literature regarding inhibition of Pseudomonas elastase. Here is an article about Pseudomonas elastase that may be a helpful reference for your research, PMCID: PMC347797, In vitro inhibition of Pseudomonas aeruginosa elastase by metal-chelating peptide derivatives.
Answered by: Technical Support
Date published: 2017-08-03
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Rated 5 out of 5 by from Masood et al Masood et al. (PubMed ID 26136527) used Sivelestat to inhibit neutrophil elastase activity to reduce lung macrophage influx into the lung after O2 exposure. -SCBT Publication Review
Date published: 2015-03-03
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