N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐

中文名称:

N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐

中文同义词:

西维来司钠;N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐

英文名称:

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

英文同义词:

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号:

150374-95-1

分子式:

C20H21N2NaO7S

分子量:

456.44

EINECS号:

相关类别:

医药原料

Mol文件:

150374-95-1.mol

熔点 

104-108 °C(Solv: water (7732-18-5))

储存条件 

Desiccate at RT

生物活性

Sivelestat (EI546) sodium 是竞争性的人类中性粒细胞弹性蛋白酶的抑制剂，其IC50 值为 44 nM， Ki 值为 200 nM。Sivelestat (EI546) sodium 有潜力用于COVID-19 的急性肺损伤/急性呼吸窘迫综合征或弥散性血管内凝血的研究。

体外研究

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.

体内研究

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.

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.