生物活性 | |||
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描述 | The complement system is a key part of the innate and adaptive immune system and plays a major role in homeostasis by clearing altered host cells and invading pathogens. Compstatin, a 13-residue peptide, is an effective inhibitor of the activation of complement component C3 with IC50 value of 12 μM and thus blocks a central and crucial step in the complement cascade[1]. In vitro studies of compstatin in human blood indicated that a major pathway of biotransformation was the removal of Ile1, which could be blocked by N-acetylation of the peptide[2]. Subsequent interaction analysis confirmed that compstatin binds NHP C3 (baboon) and human C3 with similar affinity, but it does not bind to mouse or rat C3[3]. Compstatin produced complete inhibition at a total dose of 21 mg/kg when given as a combination of bolus injection and infusion. It completely inhibited in vivo heparin/protamine-induced complement activation without adverse effects on heart rate or systemic arterial, central venous, and pulmonary arterial pressures[4]. | ||
作用机制 | The crystal structure reveals that the compstatin-binding site is formed by the macroglobulin (MG) domains 4 and 5[1]. |
细胞研究 | |||||
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细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
RPE cells | 50 uM | Function assay | Inhibition of complement activation in human fetal RPE cells assessed as reduction in C5b-9 formation at 50 uM by fluorescence assay in presence of complement-competant human serum | 25494040 |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.64mL 0.13mL 0.06mL |
3.22mL 0.64mL 0.32mL |
6.45mL 1.29mL 0.64mL |
参考文献 |
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