Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ensifentrine (Ensifentrinum) 是首创的吸入式磷酸二酯酶 3 (PDE3) 和PDE4双重抑制剂,IC50分别为 0.4 nM 和 1479 nM。它具有支气管保护和抗炎作用,可用于研究慢性阻塞性肺疾病 (COPD) 。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 997 | 现货 | ||
5 mg | ¥ 1,990 | 现货 | ||
10 mg | ¥ 3,320 | 现货 | ||
25 mg | ¥ 6,990 | 现货 | ||
50 mg | ¥ 9,420 | 现货 | ||
100 mg | ¥ 12,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 2,190 | 现货 |
产品描述 | Ensifentrine (Ensifentrinum) is a PDE3/4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis. |
靶点活性 | PDE3:0.4 nM, PDE4:1479 nM |
体外活性 | Electrical field stimulation-induced contraction of guinea pig superfused isolated tracheal preparations was significantly inhibited by Ensifentrine (10 microM) (percentage control; 93 +/- 1.2). Contractile responses were suppressed for up to 12 h after termination of superfusion with Ensifentrine demonstrating a long duration of action. Ensifentrine4 inhibited, in a concentration-dependent manner, lipopolysaccharide-induced tumor necrosis factor alpha release from human monocytes [IC50; 0.52 microM (0.38-0.69)] and proliferation of human mononuclear cells to phytohemagglutinin [IC50; 0.46 microM (0.24-0.9)][2]. |
体内活性 | Ensifentrine administered orally significantly inhibited eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs. Likewise, inhalation of dry powder containing Ensifentrine by conscious guinea pigs (25% in micronized lactose) 1.5 h before antigen exposure significantly inhibited the recruitment of eosinophils to the airways. Exposure of conscious guinea pigs to inhalation of dry powder containing Ensifentrine (2.5%) and RPL565 (25%) in micronized lactose significantly inhibited histamine-induced plasma protein extravasation in the trachea and histamine-induced bronchoconstriction over a 5.5-h period[2]. |
别名 | Ensifentrina, Ensifentrinum |
分子量 | 477.56 |
分子式 | C26H31N5O4 |
CAS No. | 1884461-72-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 20 mg/ml(41.88 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.094 mL | 10.4699 mL | 20.9398 mL | 52.3494 mL |
5 mM | 0.4188 mL | 2.094 mL | 4.188 mL | 10.4699 mL | |
10 mM | 0.2094 mL | 1.047 mL | 2.094 mL | 5.2349 mL | |
20 mM | 0.1047 mL | 0.5235 mL | 1.047 mL | 2.6175 mL |
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。
Ensifentrine 1884461-72-6 Metabolism PDE RPL 554 RPL554 inhaled Inhibitor RPL-554 bronchoprotective inhibit COPD PDE4 Ensifentrina anti-inflammatory Ensifentrinum PDE3 Phosphodiesterase (PDE) inhibitor