Compstatin

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Chemical Structure| 206645-99-0 同义名 : -
CAS号 : 206645-99-0
货号 : A773831
分子式 : C66H99N23O17S2
纯度 : 99%+
分子量 : 1550.766
MDL号 : MFCD09263618
存储条件:

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

H2O: 100 mg/mL(64.48 mM),配合低频超声助溶

动物实验配方:
生物活性
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
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
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

[1]Janssen BJ, Halff EF, Lambris JD, Gros P. Structure of compstatin in complex with complement component C3c reveals a new mechanism of complement inhibition. J Biol Chem. 2007;282(40):29241‐29247

[2]Sahu A, Soulika AM, Morikis D, Spruce L, Moore WT, Lambris JD. Binding kinetics, structure-activity relationship, and biotransformation of the complement inhibitor compstatin. J Immunol. 2000;165(5):2491‐2499

[3]Mastellos DC, Yancopoulou D, Kokkinos P, et al. Compstatin: a C3-targeted complement inhibitor reaching its prime for bedside intervention. Eur J Clin Invest. 2015;45(4):423‐440

[4]Soulika AM, Khan MM, Hattori T, et al. Inhibition of heparin/protamine complex-induced complement activation by Compstatin in baboons. Clin Immunol. 2000;96(3):212‐221