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complement C3

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库存信息

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库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
rp173717-500μg 500μg 期货 Stock Image
rp173717-1mg 1mg 期货 Stock Image

基本描述

产品名称 complement C3

产品规格参数

CAS编号和信息 rp173717

关联配体

Ligand ID 9414
名称 complement C3
类别 Peptide
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 The three principal activation pathways of the complement system (the classical, lectin and alternative pathways) converge on complement peptide C3, making it a central target for drug development in the search for immune system modulators for the treatment of complement-mediated disorders. Excessive or uncontrolled activation of the complement system plays a key role in a wide range of autoimmune and inflammatory diseases. Pharmacological inhibition of C3 activation can modify all outcomes of complement cascade activation (opsonization, inflammation and membrane attack complex formation), irrespective of which complement pathway is activated.

C3 inhibitors in development, include derivatives. Examples include Apellis Pharmaceuticals' peptide drug candidates which act as C3 inhibitors to effect disease control and disease modification, in conditions including paroxysmal nocturnal hemoglobinuria (PNH), age-related macular degeneration (AMD) and chronic obstructive pulmonary disease (COPD). APL-1 (previously POT-4), a short-acting inhibitor has completed Phase 1 in AMD and has potential for COPD (inhaled administration). APL-2 (INN pegcetacoplan; FDA approved 2021 as Empaveli®) is PEGylated APL-1 formulated for subcutaneous (PNH) and intravitreal administration (AMD). Pegcetacoplan was the first C3-targeted PNH therapy to be approved in the USA. APL-9 (a second generation derivative of APL-2) was tested in clinical trial for potential to treat SARS-CoV-2-induced mild-moderate ARDS (NCT04402060), but the program was terminated in early 2021 when an interim data review showed that APL-9 therapy did not significantly reduce mortality.

AMY-101 (a next-generation proprietary compstatin from Amyndas Pharmaceuticals) has been granted Orphan Designation by both the EMA and US FDA for the treatment of C3 glomerulopathy (C3G). This candidate has been entered into clinical trials that aim to determine its ability to combat the inflammatory damage (to lung and other organs) in patients with severe COVID-19 (Phase 2 NCT04395456) . Peptide Cp40 has shown effective C3 inhibition in C3G in vitro .
配体家族 Complement components and ligands
基因/前体
Gene symbol Gene name Precursor protein name Species 别名
C3 complement C3 prepro-C3 Human CPAMD1, complement component 3
单字母多肽序列 SPMYSIITPNILRLESEETMVLEAHDAQGDVPVTVTVHDFPGKKLVLSSEKTVLTPATNHMGNVTFTIPANREFKSEKGRNKFVTVQATFGTQVVEKVVLVSLQSGYLFIQTDKTIYTPGSTVLYRIFTVNHKLLPVGRTVMVNIENPEGIPVKQDSLSSQNQLGVLPLSWDIPELVNMGQWKIRAYYENSPQQVFSTEFEVKEYVLPSFEVIVEPTEKFYYIYNEKGLEVTITARFLYGKKVEGTAFVIFGIQDGEQRISLPESLKRIPIEDGSGEVVLSRKVLLDGVQNPRAEDLVGKSLYVSATVILHSGSDMVQAERSGIPIVTSPYQIHFTKTPKYFKPGMPFDLMVFVTNPDGSPAYRVPVAVQGEDTVQSLTQGDGVAKLSINTHPSQKPLSITVRTKKQELSEAEQATRTMQ
三字母多肽序列
翻译后修饰
化学修饰

参考文献

1. Zhang Y, Shao D, Ricklin D, Hilkin BM, Nester CM, Lambris JD, Smith RJ.  (2015)  Compstatin analog Cp40 inhibits complement dysregulation in vitro in C3 glomerulopathy..  Immunobiology,  220  (8):  (993-8).  [PMID:25982307]
2. Kajikawa T, Briones RA, Resuello RRG, Tuplano JV, Reis ES, Hajishengallis E, Garcia CAG, Yancopoulou D, Lambris JD, Hajishengallis G.  (2017)  Safety and Efficacy of the Complement Inhibitor AMY-101 in a Natural Model of Periodontitis in Non-human Primates..  Mol Ther Methods Clin Dev,  (13):  (207-215).  [PMID:28879212]
3. Mastaglio S, Ruggeri A, Risitano AM, Angelillo P, Yancopoulou D, Mastellos DC, Huber-Lang M, Piemontese S, Assanelli A, Garlanda C et al..  (2020)  The first case of COVID-19 treated with the complement C3 inhibitor AMY-101..  Clin Immunol,  215  (13):  (108450).  [PMID:32360516]

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