Sivelestat Sodium tetrahydrate

Modify Date: 2024-01-03 16:00:23

Sivelestat Sodium tetrahydrate Structure
Sivelestat Sodium tetrahydrate structure
Common Name Sivelestat Sodium tetrahydrate
CAS Number 201677-61-4 Molecular Weight 528.506
Density N/A Boiling Point N/A
Molecular Formula C20H29N2NaO11S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Sivelestat Sodium tetrahydrate


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 sodium,2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate,tetrahydrate
Synonym More Synonyms

 Sivelestat Sodium tetrahydrate 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

Molecular Formula C20H29N2NaO11S
Molecular Weight 528.506
Exact Mass 528.138977
PSA 187.00000
LogP 2.20610
Storage condition -20℃

 Synonyms

Propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester, sodium salt, hydrate (1:1:4)
Sivelestat sodium hydrate
Sivelestat Sodium
Sivelestat sodium tetrahydrate
Elaspol
ONO-5046.Na
(N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycinato-κO)sodium tetrahydrate
Sodium ({2-[({4-[(2,2-dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}amino)acetate hydrate (1:1:4)
sodium, [2,2-dimethylpropanoato, 4-[[[2-[[[(carboxy-κO)methyl]amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester]-, hydrate (1:4)
MFCD01937969
UNII-737RR8Y409
Sivelestat (sodium tetrahydrate)
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