西维来司钠 ≥98%
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| 包装规格: | 5mg 10mg 25mg 50mg 100mg in glass bottle |
| 溶解性: | 溶于DMSO(100 mg/mL 超声) |
| 产品描述: | 基本信息 产品编号:S10650 产品名称:Sivelestat sodium CAS: 150374-95-1 储存条件 粉末 -20℃ 四年 分子式: C20H21N2NaO7S 溶于液体 -80℃ 六个月 分子量 456.44 -20℃ 一个月 化学名: sodium;2-[[2-[[4-(2,2-dimethylpropanoyloxy)phenyl]sulfonylamino]benzoyl]amino]acetate Solubility (25°C) 体外 DMSO 100mg/mL (219.09mM; Need ultrasonic) Ethanol Water 1mg/mL (2.19mM; ultrasonic and warming ) 体内 现配现用 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 2.1909mL 10.9543mL 21.9087mL 5mM 0.4382mL 2.1909mL 4.3817mL 10mM 0.2191mL 1.0954mL 2.1909mL 生物活性 产品描述 一种竞争性的人类中性粒细胞弹性蛋白酶的抑制剂,其IC50 值为 44nM, Ki 值为 200nM。 靶点/IC50 Elastase SARS-CoV 体外研究 Sivelestat (ONO-5046) does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100μM. Sivelestat (ONO-5046) exhibits IC50 values of 44nM, 36nM, 19nM, 37nM and 49nM for human, rabbit, rat, hamster and mouse neutrophil elastase, respectively. 体内研究 Sivelestat (ONO-5046, 0.021-2.1mg/kg, intratracheally) suppresses lung hemorrhage in hamster (ID50 = 82pg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6mg/kg) by intravenous administration, both of which are induced by human neutrophil elastase. Sivelestat (10mg/kg, infusion via the tail vein) ameliorates lung injury after hemorrhagic shock in rats. Sivelestat (15, 60mg/kg,ip) prevents ischemia–reperfusion injury in the rat bladder. Animal Model: Male Golden hamsters, weighing 90 to 110g Dosage: 0.021-2.1mg/kg. Administration: Intratracheally five min before HNE injection. Result: Significantly and dosedependently suppressed the lung hemorrhage. Animal Model: Male Sprague-Dawley rats weighing 350-400g Dosage: 10mg/kg. Administration: Continuous infusion via the tail vein at 10 mg/kg/h for 60min 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 250-320g Dosage: 15mg/kg or 60mg/kg Administration: IP. Result: Decreased the blood flow in the bladder during reperfusion phase compared to the IR group. |
| 保存条件: | -20℃ |
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