|2-((4R,7S,10S,13S,19S,22S,25S,28S,31S,34R)-10,13-双((1H-咪唑-4-基)甲基)-19-((1H-吲哚-3-基)甲基)-4-(((2S,3R)-1-氨基-3-羟基-1-氧代丁-2-基)氨基甲酰基)-34-((2S,3S)-2-氨基-3-甲基戊酰胺)-25-(3-氨基-3-氧代丙基)-7-(3-胍基丙基)-28,31-二异丙基-6,9,12,15,18,21,24,27,30,33-十氧代-1,2-二硫杂-5,8,11,14,17,20,23,26,29,32-十氮杂环三十五烷-22-基)乙酸|CsnPharm

CAS No.: 206645-99-0

Compstatin/坎普他汀 Catalog No. CSN23354

Synonyms: 坎普他汀

Compstatin is a complement inhibitor which can bind C3 inhibiting proteolytic cleavage by C3 convertase with IC50 value of 28 μM and activate classical and alternative complement pathways with IC50 values of 63 and 12 μM, respectively.

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技术信息

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.6448 mL
- 3.2242 mL
- 6.4484 mL
- 5 mM
- 0.1290 mL
- 0.6448 mL
- 1.2897 mL
- 10 mM
- 0.0645 mL
- 0.3224 mL
- 0.6448 mL

技术信息

CAS号	206645-99-0	储存条件	粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C66H99N23O17S2	运输	蓝冰
分子量	1550.77	别名	坎普他汀

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