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N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt

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N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt Basic information

Product Name:
N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt
Synonyms:
  • n-[2-[[[4-(2,2-dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(s)-glycine monosodium salt
  • SIVELESTAT SODIUM
  • N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycinesodiumsalt
  • Sivelestat sodium salt
  • Glycine, N-[2-[[[4-(2,2-diMethyl-1-oxopropoxy)phenyl]sulfonyl]aMino]benzoyl]-, MonosodiuM salt
  • Sivelestat SodiuM anhydrous
  • sodium,2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate
  • sodium 2-[[[2-[[4-(2,2-dimethyl-1-oxopropoxy)phenyl]sulfonylamino]phenyl]-oxomethyl]amino]acetate
CAS:
150374-95-1
MF:
C20H21N2NaO7S
MW:
456.44
Product Categories:
  • GYL
Mol File:
150374-95-1.mol
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N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt Chemical Properties

Melting point:
104-108 °C(Solv: water (7732-18-5))
storage temp. 
Desiccate at RT
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Solid
color 
White to Off-White
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N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt Usage And Synthesis

Uses

Treatment of acute lung injury; acute respiratory distress syndrome (elastase inhibitor).

Uses

Sivelestat Sodium is an inhibitor of neutrophil elastase. Also, it is a promising therapeutic agent for severe acute pneumonitis caused by gefitinib.

Biological Activity

Selective leukocyte elastase inhibitor (IC 50 = 44 nM) that displays no activity at a range of other proteases. Inhibits NF- κ B activation and LTB 4 -induced neutrophil transmigration in vitro . Significantly attenuates ischemia-induced spinal cord injury, decreases serum cytokine levels and reduces acute inflammatory lung injury in vivo .

in vivo

Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID50 = 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase[1].
Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats[2].
Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder[3].

Animal Model:Male Golden hamsters, weighing 90 to 110 g[1].
Dosage:0.021-2.1 mg/kg.
Administration:Intratracheally five min before HNE injection.
Result:Significantly and dosedependently suppressed the lung hemorrhage.
Animal Model:Male Sprague-Dawley rats weighing 350-400 g[2].
Dosage:10 mg/kg.
Administration:Continuous infusion via the tail vein at 10 mg/kg/h for 60 min during the resuscitation phase.
Result:Greatly suppressed lung injury, as revealed by the reduced histological damage.
Significantly ameliorated HSR-induced lung injury.
Markedly decreased the levels of TNF-α and iNOS gene.
Animal Model:Male Sprague Dawley rats, 8 weeks old and weighing 250-320 g[3].
Dosage:15 mg/kg or 60 mg/kg.
Administration:IP.
Result:Decreased the blood flow in the bladder during reperfusion phase compared to the IR group.

storage

Desiccate at RT

N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium saltSupplier

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