| Description | Zilucoplan TFA (RA101495), a 15-amino acid macrocyclic peptide, serves as a potent inhibitor of complement component 5 (C5). It has applications in the study of immune-mediated necrotising myopathy (IMNM) [1] [2]. |
| In vitro | Zilucoplan (RA101495; 1-1000 nM; 30分钟) 抑制脂多糖诱导的人全血中C5a血浆水平增加，IC50值为474.5 pM。在1 nM浓度下观察到C5a血浆水平有65.7%的降低[2]。Zilucoplan与补体成分5（C5）结合，通过抑制C5转化酶对C5的切割，阻止C5a和C5b的产生，且与已形成的C5b结合从而立体阻碍其与C6的相互作用，从而抑制膜孔的形成和继发的细胞死亡，阻断膜攻击复合体（MAC; C5b-9）的下游组装[1]。 |
| In vivo | Zilucoplan (RA101495; 10 mg/kg; S.C.; 每日, 连续6天) 能够阻止C5缺陷小鼠在加入人类补体后发展成免疫介导的坏死性肌病 (IMNM) [1]。同样的剂量和给药方式在保护C57BL/6小鼠免受肌病的效果上也显示出效力 [1]。 |
| Synonyms | RA101495 TFA |
| molecular weight | 3562.18 (free base) |
| Molecular formula | (C2H4O)nC126H186N24O32.C2HF3O2 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |