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
- 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
- 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。
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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.
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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.
- 更新日期:2024/11/08
- 产品编号:HY-17443A
- 产品名称:Sivelestat sodium
- CAS编号:
- 包装:5 mg
- 价格:437元
- 更新日期:2024/11/08
- 产品编号:HY-17443A
- 产品名称: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 Sivelestat sodium
- CAS编号:150374-95-1
- 包装:10mg
- 价格:700元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5726
- 优势度:77