Powder: -20°C for 3 years | In solvent: -80°C for 1 year
W-54011 是口服有效的非肽 C5a 受体拮抗剂,抑制125I 标记的 C5a 与人嗜中性白细胞的结合,Ki 为 2.2 nM。它还抑制C5a 诱导的人嗜中性粒细胞的细胞内 Ca2+动员,趋化性和ROS 的生成,IC50分别为 3.1 nM、2.7 nM 和1.6 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 691 | 现货 | ||
5 mg | ¥ 1,410 | 现货 | ||
10 mg | ¥ 2,130 | 现货 | ||
25 mg | ¥ 3,590 | 现货 | ||
50 mg | ¥ 5,190 | 现货 | ||
100 mg | ¥ 7,360 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,490 | 现货 |
产品描述 | W-54011 is a potent non-peptide C5a receptor antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils (Ki = 2.2 nM). W-54011 inhibits C5a-induced intracellular Ca2+ mobilization, chemotaxis, and generation of ROS in human neutrophils (IC50s = 3.1 nM, 2.7 nM, and 1.6 nM, respectively). |
靶点活性 | Chemotaxis:2.7 nM(ki), Ca2+ mobilization: 3.1 nM, complement 5a receptor (C5aR):2.2 nM(Ki), ROS:1.6 nM(ki) |
体外活性 | W-54011 does not show agonistic activity at up to 10 μM and shifts rightward the concentration-response curves to C5a without depressing the maximal responses, showing that W-54011 is a full antagonist. At concentrations up to 10 μM, W-54011 does not affect Ca2+ mobilization stimulated with sub-maximally effective concentrations of fMLP (1 nM), platelet-activating factor (0.3 nM), and IL-8 (0.1 nM)[1]. |
体内活性 | W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils (IC50 = 1.7 nM and 3.2 nM, respectively). In Male mongolian gerbils injected with rhC5a, W-54011 (3-30 mg/kg; oral; for 4 hours) inhibited C5a-induced neutropenia in a dose-dependent manner in gerbils. The species selectivity of W-54011 is examined in rhC5a-induced intracellular Ca2+ mobilization of neutrophils in various species [1]. |
分子量 | 493.08 |
分子式 | C30H37ClN2O2 |
CAS No. | 405098-33-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 28 mg/mL (56.79 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0281 mL | 10.1403 mL | 20.2807 mL | 50.7017 mL |
5 mM | 0.4056 mL | 2.0281 mL | 4.0561 mL | 10.1403 mL | |
10 mM | 0.2028 mL | 1.014 mL | 2.0281 mL | 5.0702 mL | |
20 mM | 0.1014 mL | 0.507 mL | 1.014 mL | 2.5351 mL | |
50 mM | 0.0406 mL | 0.2028 mL | 0.4056 mL | 1.014 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。
W-54011 405098-33-1 Immunology/Inflammation ROS Complement System W54011 chemotaxis inhibit orally W 54011 mobilization anaphylatoxin Reactive Oxygen Species Ca2+ C5a neutrophils Inhibitor inflammatory inhibitor