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

生物活性体外研究体内研究 N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐试剂级价格

CAS号:150374-95-1
英文名:N-[2-[[[4-(2,2-Dimethyl-1-oxopropoxy)phenyl]sulfonyl]amino]benzoyl]-(S)-glycine monosodium salt
中文名: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
CBNumber:CB02131171
分子式:C20H21N2NaO7S
分子量:456.44
MOL File:150374-95-1.mol

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

熔点 :104-108 °C(Solv: water (7732-18-5))
储存条件 :Desiccate at RT
溶解度 :DMSO (Slightly), Methanol (Slightly)
形态 :Solid
颜色 :White to Off-White

N-[2-[[[4-(2,2-二甲基-1-氧代丙氧基)苯基]磺酰]氨基]苯甲酰]-(S)-甘氨酸单钠盐性质、用途与生产工艺

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.