Sivelestat sodium salt hydrate

Names

[ Name ]:
Sivelestat sodium salt hydrate

[Synonym ]:
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

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

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℃

MSDS

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Safety Information

[ HS Code ]:
2935009090

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

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%