| 名称 | W-54011 |
| 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). |
| 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]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 28 mg/mL (56.79 mM)
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| 关键字 | W54011 | chemotaxis | inhibit | orally | W 54011 | mobilization | anaphylatoxin | ROS | Reactive Oxygen Species | Ca2+ | C5a | neutrophils | Inhibitor | Complement System | W-54011 | inflammatory |
| 相关产品 | (±)-Catechin | Allopurinol | Acetylcysteine | Tempol | Inosine | Lycopene | Ethyl cinnamate | Baicalein | Rifamycin S | Cyclosporin A | 3-Phenoxybenzaldehyde | Gallic acid |
| 相关库 | NF-κB 通路分子库 | 经典已知活性库 | 细胞焦亡化合物库 | 抗氧化化合物库 | 抑制剂库 | 线粒体靶向库 | 代谢化合物库 | 口服活性化合物库 | 抗衰老化合物库 | 已知活性化合物库 |
United States
