N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt
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
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
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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N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt(150374-95-1)Related Product Information
- ETHANE
- Chlorodimethylphenylsilane
- 4-Hydroxy-D-(-)-2-phenylglycine
- Benzoyl chloride
- Dimethyl sulfoxide
- Dimethyldimethoxysilane
- Sulfuryl chloride
- Sodium hydroxide
- Sodium citrate
- Sivelestat
- Sodium sulfate
- BENZOYL ISOCYANATE
- Dimethyl fumarate
- Diclofenac sodium
- Imipenem-Cilastatin sodium hydrate
- Diethoxydimethylsilane
- Montelukast sodium
- Sodium benzoate