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Sivelestat Sodium tetrahydrate

Names

[ CAS No. ]:
201677-61-4

[ Name ]:
Sivelestat Sodium tetrahydrate

[Synonym ]:
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)

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]:

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 | Alvelestat | Sivelestat sodium salt hydrate | AE-3763 | BAY 678 | BAY-85-8501 | Lodelaben | ZD-0892 | ZD8321

Chemical & Physical Properties

[ Molecular Formula ]:
C20H29N2NaO11S

[ Molecular Weight ]:
528.506

[ Exact Mass ]:
528.138977

[ PSA ]:
187.00000

[ LogP ]:
2.20610

[ Storage condition ]:
-20℃

Related Compounds