Sivelestat sodium salt hydrate

Modify Date: 2024-01-03 19:15:21

Sivelestat sodium salt hydrate Structure
Sivelestat sodium salt hydrate structure
Common Name Sivelestat sodium salt hydrate
CAS Number 127373-66-4 Molecular Weight 434.463
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C20H22N2O7S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Sivelestat sodium salt hydrate


Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2].

 Names

Name 2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetic acid
Synonym More Synonyms

 Sivelestat sodium salt hydrate Biological Activity

Description Sivelestat(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse.IC50 value: 44 nM [1]Target: neutrophil elastaseONO-5046 did not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 microM. In in vivo studies, ONO-5046 suppressed lung hemorrhage in hamster (ID50 = 82 micrograms/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase [1]. Sivelestat sodium hydrate is an anti-neutrophil elastase inhibitor and may be one of the treatment options for acute respiratory failure due to pneumocystis pneumonia in AIDS patients [2].
Related Catalog
References

[1]. Kawabata K, et al. ONO-5046, a novel inhibitor of human neutrophil elastase. Biochem Biophys Res Commun. 1991 Jun 14;177(2):814-20.

[2]. Imokawa S, et al. Acute respiratory failure due to pneumocystis pneumonia successfully treated with combined use of sivelestat sodium hydrate. Nihon Kokyuki Gakkai Zasshi. 2008 Jun;46(6):461-5.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C20H22N2O7S
Molecular Weight 434.463
Exact Mass 434.114777
PSA 147.25000
LogP 2.96
Index of Refraction 1.598
Storage condition -20℃

 Safety Information

HS Code 2935009090

 Customs

HS Code 2935009090
Summary 2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

 Synonyms

N-(2-(((4-(2,2-Dimethyl-1-oxopropoxy)phenyl)sulfonyl)amino)benzoyl)glycine
o-(p-Hydroxybenzenesulfonamido)hippuric Acid Pivalate (Ester)
Sivelestat
Propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester
ONO5046
Sivelestat sodium salt hydrate
EI 546
Elastase Inhibitor IV
N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycine