c5ar 1

C5aR1 antagonist peptide 是一种源自C5a (趋化因子补体片段5过敏毒素) C末端的生物活性线性肽。它能在人和大鼠的C5a受体上阻断C5a的结合，对于细胞免疫反应的触发起着关键作用。C5a的过度表达与多种免疫炎性疾病如关节炎、阿尔茨海默病、囊性纤维化和系统性红斑狼疮等有着密切关联。

C5aR1 antagonist 2 (Compound 6a) 为口服活性的 C5a 受体1 (C5aR1) 拮抗剂，专门用于抑制中性粒细胞计数因 C5a 诱导而增加。在 DISCO 和迁移测定中表现出高效的抑制作用，IC50 值为 21 nM 和 3 nM。C5aR1 antagonist 2 适用于急慢性炎症性疾病的相关研究。

C5aR-IN-1 是一种有效的C5aR 抑制剂。C5a 水平升高与自身免疫性疾病和炎症性疾病等疾病有关。C5aR-IN-1 具有研究炎症性疾病的潜力。

Vilobelimab (CaCP-29) 是一种靶向人补体成分 5a 的人鼠嵌合 IgG 抗体，是一种 C5a 抑制剂，抑制中性粒细胞活化，可用于研究 SARS-CoV-2 感染引起的全身炎症。

PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activityMol. Pharmacol.65(4)868-879(2004) 2.Jain, U., Woodruff, T.M., and Stadnyk, A.W.The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10Br. J. Pharmacol.168(2)488-501(2013) 3.Staab, E.B., Sanderson, S.D., Wells, S.M., et al.Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthmaInt. Immunopharmacol.21(2)293-300(2014) 4.Fonseca, M.I., Ager, R.R., Chu, S.-H., et al.Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's diseaseJ. Immunol.183(2)1375-1383(2009)