| Identification | Back Directory | [Name]
N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt | [CAS]
150374-95-1 | [Synonyms]
SIVELESTAT SODIUM
Sivelestat sodium salt
Sivelestat SodiuM anhydrous
sodium,2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate
N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycinesodiumsalt
Glycine, N-[2-[[[4-(2,2-diMethyl-1-oxopropoxy)phenyl]sulfonyl]aMino]benzoyl]-, MonosodiuM salt
n-[2-[[[4-(2,2-dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(s)-glycine monosodium salt
sodium 2-[[[2-[[4-(2,2-dimethyl-1-oxopropoxy)phenyl]sulfonylamino]phenyl]-oxomethyl]amino]acetate
N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt USP/EP/BP | [Molecular Formula]
C20H21N2NaO7S | [MOL File]
150374-95-1.mol | [Molecular Weight]
456.44 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
Treatment of acute lung injury; acute respiratory distress syndrome (elastase inhibitor). | [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.
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| 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 |
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