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Sivelestat Sodium

Names

[ CAS No. ]:
150374-95-1

[ Name ]:
Sivelestat Sodium

[Synonym ]:
Propanoic acid, 2,2-dimethyl-, 4-[[[2-[[(carboxymethyl)amino]carbonyl]phenyl]amino]sulfonyl]phenyl ester, sodium salt (1:1)
Sivelestat Sodium
UNII:0CLL4232KD
HMS3262D11
Sivelestat sodium anhydrous
Sivelestat sodium salt hydrate
Sodium ({2-[({4-[(2,2-dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}amino)acetate
ONO-5046.Na
Sivelestat sodium salt
Sivelestat (sodium)

Biological Activity

[Description]:

Sivelestat sodium(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]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase
Research Areas >> Others

[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.


[Related Small Molecules]

DMP 777 | GW311616 | Sivelestat Sodium tetrahydrate | Alvelestat | AE-3763 | BAY 678 | BAY-85-8501 | Lodelaben | ZD-0892 | ZD8321

Chemical & Physical Properties

[ Molecular Formula ]:
C20H21N2NaO7S

[ Molecular Weight ]:
456.445

[ Exact Mass ]:
456.096710

[ PSA ]:
150.08000

[ LogP ]:
2.46330

[ Storage condition ]:
Desiccate at RT

Related Compounds