Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SSR69071 是一种有效的,具有口服活性的选择性中性粒细胞弹性蛋白酶 (neutrophil elastase) 抑制剂。SSR69071 对人弹性蛋白酶 (Ki=0.0168 nM) 的亲和力高于对大鼠 (Ki=3 nM)、小鼠 (Ki=1.8 nM) 和兔 (Ki=58 nM) 弹性蛋白酶。SSR69071 减少缺血再灌注损伤后的心肌梗死面积。SSR69071 还具有治疗慢性阻塞性肺病、哮喘、肺气肿、囊性纤维化和多种炎症性疾病的潜力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 560 | 35日内发货 | ||
5 mg | ¥ 2,130 | 35日内发货 | ||
10 mg | ¥ 3,940 | 35日内发货 |
产品描述 | SSR69071 is a potent, orally active, and selective inhibitor of neutrophil elastase. SSR69071 displays a higher affinity for human elastase (Ki =0.0168 nM) than for rat (Ki =3 nM), mouse (Ki =1.8 nM), and rabbit (Ki = 58 nM) elastases [2]. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury [1]. SSR69071 also has the potential for the treatment of chronic obstructive pulmonary diseases, asthma, emphysema, cystic fibrosis, and several inflammatory diseases. |
体外活性 | SSR69071 is a potent inhibitor of human leukocyte elastase (HLE), with the inhibition constant (K i ) and the inactivation process constant (k on ) of 0.0168±0.0014 nM and 0.183±0.013 10 6 /mol sr, respectively [2]. SSR69071 is a potent, competitive and slow tight binding inhibitor of HLE in vitro with a Ki value of 16.8 pM [3]. |
体内活性 | SSR69071 (3 mg/kg i.v.) reduces cardiac infarct size when administered before ischemia or just prior to reperfusion (−37%, P<0.05)[1]. Treatment with SSR69071 (3 mg/kg i.v.) just prior to reperfusion significantly reduces cardiac elastase activity [1]. Bronchoalveolar lavage fluid from mice orally treated with SSR69071 inhibits HLE (ex vivo), and in this model, SSR69071 has a dose-dependent efficacy with an ED 50 =10.5 mg/kg p.o. SSR69071 decreases significantly the acute lung hemorrhage induced by HLE (ED 50 =2.8 mg/kg p.o.) in mice [2]. SSR69071 prevents carrageenan- (ED 30 =2.2 mg/kg) and HLE-induced (ED 30 =2.7 mg/kg) paw edema in rats after p.o. administration [2]. Animal Model: Male New Zealand white rabbits weighing 2-3 kg [1] Dosage: 3 mg/kg (dissolved in methane sulphonic acid before being diluted in 0.9% saline) Administration: Administered i.v. Result: Treatment just prior to reperfusion significantly reduced cardiac elastase activity. |
分子量 | 556.63 |
分子式 | C27H32N4O7S |
CAS No. | 344930-95-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
SSR 69071 344930-95-6 SSR69071 SSR-69071 Inhibitor inhibitor inhibit