Certolizumab pegol
(Synonyms: 赛妥珠单抗,Certolizumab; CDP870) 目录号 : GC65487Certolizumab pegol(Certolizumab)是一种重组、聚乙烯糖基化、抗原结合片段的人源化单克隆抗体,选择性靶向和中和肿瘤坏死因子-α(TNF-α)。Certolizumab pegol可用于类风湿关节炎和克罗恩病研究。
Cas No.:428863-50-7
Sample solution is provided at 25 µL, 10mM.
Certolizumab pegol (Certolizumab) is a recombinant, polyethylene glycolylated, antigen-binding fragment of a humanized monoclonal antibody that selectively targets and neutralizes tumour necrosis factor-α (TNF-α). Certolizumab pegol can be used for rheumatoid arthritis and Crohn disease research[1-2].
Certolizumab pegol neutralizes soluble TNF-α with an IC90 of 3ng/mL. Preincubation of human monocytes with certolizumab pegol at concentrations of 1μg/mL and above completely inhibited lipopolysaccharide(LPS)-induced IL-1β production, and certolizumab pegol did not induce apoptosis of activated human monocytes or peripheral blood lymphocytes (PBLs), nor did it cause changes in the integrity of polymorphonuclear granules (PMNs)[2]. In addition, certolizumab pegol can directly induce non-apoptotic cell death in transmembrane TNF-α-expressing cells[4].
Certolizumab pegol (10μg, single dose) reduced the severity of acute pancreatitis, and serum amylase, lipase, and lactate dehydrogenase levels were significantly reduced in the certolizumab pegol-treated group[3]. Compared with the control group (non-inflamed tissue), certolizumab pegol (2mg/kg) can effectively penetrate into the inflamed arthritic paws of mice and improve arthritis in mice[5].
References:
[1] Deeks ED. Certolizumab pegol: a review of its use in the management of rheumatoid arthritis. Drugs. 2013 Jan;73(1):75-97.
[2] Nesbitt A, et al. Mechanism of action of certolizumab pegol (CDP870): in vitro comparison with other anti-tumor necrosis factor alpha agents. Inflamm Bowel Dis. 2007 Nov;13(11):1323-32.
[3] Kosekli M A, Sungurtekin U, Cobankara V, et al. Effects of certolizumab on cerulein-induced acute pancreatitis in rats[J]. Pancreas, 2016, 45(8): 1120-1125.
[4] Ueda N, Tsukamoto H, Mitoma H, et al. The cytotoxic effects of certolizumab pegol and golimumab mediated by transmembrane tumor necrosis factor α[J]. Inflammatory bowel diseases, 2013, 19(6): 1224-1231.
[5] Palframan R, Airey M, Moore A, et al. Use of biofluorescence imaging to compare the distribution of certolizumab pegol, adalimumab, and infliximab in the inflamed paws of mice with collagen-induced arthritis[J]. Journal of immunological methods, 2009, 348(1-2): 36-41.
Certolizumab pegol(Certolizumab)是一种重组、聚乙烯糖基化、抗原结合片段的人源化单克隆抗体,选择性靶向和中和肿瘤坏死因子-α(TNF-α)。Certolizumab pegol可用于类风湿关节炎和克罗恩病研究[1-2]。
Certolizumab pegol可中和可溶性TNF-α,IC90为3ng/mL。人单核细胞与浓度为1μg/mL及以上浓度的Certolizumab pegol预孵育完全抑制了脂多糖(LPS)诱导的IL-1β的产生,并且Certolizumab pegol不会诱导活化的人单核细胞或外周血淋巴细胞(PBL)凋亡,也不会导致多形核颗粒(PMN)完整性发生变化[2]。此外,Certolizumab pegol可以直接诱导跨膜TNF-α表达细胞中的非凋亡细胞死亡[4]。
Certolizumab pegol(10μg,单剂量)可降低急性胰腺炎的严重程度,并且Certolizumab pegol治疗组血清淀粉酶、脂肪酶和乳酸脱氢酶水平显著降低[3]。与对照组相比(非炎症组织),Certolizumab pegol(2mg/kg)能有效地渗透小鼠发炎的关节炎爪子,改善小鼠关节炎[5]。
Cell experiment [1]: | |
Cell lines | Human dermal microvascular endothelial cells (HMVECs) |
Preparation Method | HMVECs was stimulated with TNF-α (25ng/ml) for 24 hours in the presence or absence of varying concentrations of certolizumab pegol or Ms-Ig. The cell culture supernatant was collected and the level of HMVEC chemokines was detected by elisa. |
Reaction Conditions | 0-10μg/mL, 24h |
Applications | Certolizumab pegol inhibits TNF-α-induced increases in angiogenic chemokines in a dose-dependent manner. |
Animal experiment [2]: | |
Animal models | Rat model of acute edematous pancreatitis |
Preparation Method | Healthy Wistar Albino male rats (n = 36) were randomly divided into 4 groups (9 rats in each group): group 1, control group; group 2, Certolizumab pegol group; group 3, cerulein group; and group 4, cerulein + Certolizumab pegol group. |
Dosage form | 10μg, single dose, i.p. |
Applications | Certolizumab pegol reduced the severity of acute pancreatitis, and serum amylase, lipase and lactate dehydrogenase levels were significantly reduced in the certolizumab pegol-treated group. |
References: |
Cas No. | 428863-50-7 | SDF | Download SDF |
别名 | 赛妥珠单抗,Certolizumab; CDP870 | ||
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