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W-54011

CAS No. : 405098-33-1

MCE 站：W-54011

产品活性：W-54011 是一种有效的，具有口服活性的非肽 C5a 受体拮抗剂。W-54011 抑制 ¹²⁵I 标记的 C5a 与人嗜中性白细胞的结合，K_i 值为 2.2 nM。W-54011 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 值分别为 3.1 nM、2.7 nM 和1.6 nM。

研究领域：Immunology/Inflammation  |  NF-κB  |  Metabolic Enzyme/Protease

作用靶点：Complement System  |  Reactive Oxygen Species

In Vitro: In C5a-induced intracellular Ca²⁺ mobilization assay with human neutrophils, 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, indicating 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), plateletactivating factor (0.3 nM), and IL-8 (0.1 nM). This result demonstrates that W-54011 is highly specific for C5a receptor.

In Vivo: W-54011 (3-30 mg/kg; oral administration; for 4 hours; male mongolian gerbils) treatment 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. The W-54011 is able to inhibit the response in cynomolgus monkeys and gerbils with IC₅₀ values of 1.7 nM and 3.2 nM, respectively, but not in mice, rats, guinea pigs, rabbits, and dogs.

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