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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;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;N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt USP/EP/BP | | CAS: | 150374-95-1 | | MF: | C20H21N2NaO7S | | MW: | 456.44 | | EINECS: | | | Product Categories: | GYL | | Mol File: | 150374-95-1.mol | ![N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt Structure](CAS/GIF/150374-95-1.gif) |
| | 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 |
| | N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt Usage And Synthesis |
| Uses | Sivelestat Sodium is an inhibitor of neutrophil elastase. Also, it is a promising therapeutic agent for severe acute pneumonitis caused by gefitinib. | | 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 |
| | N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt Preparation Products And Raw materials |
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