Avacopan 是一种口服小分子 C5aR (IC50: 0.1 nM.) 拮抗剂，可阻断 C5a 的作用并防止 AAV 小鼠模型中抗髓过氧化物酶抗体诱导的 GN 发展。

Avacopan is an orally administered small-molecule C5aR ( IC50 : 0.1 nM.)antagonist that blocks the effects of C5a and prevents the development of GN induced by anti-myeloperoxidase antibodies in a murine model of AAV.

CCX168 (avacopan), an orally administered selective and potent C5aR inhibitor.?CCX168 blocked the C5a binding, C5a-mediated migration, calcium mobilization, and CD11b upregulation in U937 cells as well as in freshly isolated human neutrophils.?CCX168 retains high potency when present in human blood.?A transgenic human C5aR knock-in mouse model allowed comparison of the in vitro and in vivo efficacy of the molecule.?CCX168 effectively blocked migration in in vitro and ex vivo chemotaxis assays, and it blocked the C5a-mediated neutrophil vascular endothelial margination.?CCX168 was effective in migration and neutrophil margination assays in cynomolgus monkeys[1].

1346623-17-3

C33H35F4N3O2

581.656

CCX168

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years