150374-95-1
150374-95-1 結(jié)構(gòu)式
基本信息
N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸單鈉鹽
Sivelestat sodium salt
Sivelestat SodiuM anhydrous
N-{2-[({4-[(2,2-Dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycinesodiumsalt
sodium,2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate
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
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM.
Sivelestat (ONO-5046) exhibits IC
50
values of 44 nM, 36 nM, 19 nM, 37 nM and 49 nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively.
Sivelestat (ONO-5046, 0.021-2.1 mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID
50
= 82 pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID
50
= 9.6 mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase.
Sivelestat (10 mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats.
Sivelestat (15, 60 mg/kg, ip) prevents ischemia–reperfusion injury in the rat bladder.
| Animal Model: | Male Golden hamsters, weighing 90 to 110 g. |
| 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. |
| 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. |
| 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. |