150374-95-1

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

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

CAS 150374-95-1

分子式 C20H21N2NaO7S

分子量 456.44

MOL 文件 150374-95-1.mol

更新日期 2024/07/05 17:12:03

150374-95-1 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

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

英文别名

SIVELESTAT SODIUM
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

所属类别

生物化工：甘氨酸类衍生物

物理化学性质

熔点104-108 °C(Solv: water (7732-18-5))

储存条件Desiccate at RT

溶解度可溶于DMSO（少许）、甲醇（少许）

形态固体

颜色白色至灰白色

常见问题列表

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.