Reslizumab
(Synonyms: Sch 55700) 目录号 : GC39430
Reslizumab是一种靶向IL-5分子的人源化IgG4/κ单克隆抗体,Kd值为81pM。
Cas No.:241473-69-8
Sample solution is provided at 25 µL, 10mM.
Reslizumab is a humanized IgG4/κ monoclonal antibody that targets IL-5 molecules, with the Kd value of 81pM[1]. Reslizumab binds to the α chain of the IL-5 receptor on the surface of eosinophils, thereby inhibiting the proliferation of eosinophils, Reslizumab can be metabolized through enzymatic protein hydrolysis into small peptides and amino acids[2]. Reslizumab has been widely used in animal models of asthma to control asthma symptoms and improve lung function[3].
In vitro, Reslizumab significantly inhibited the proliferation of TF-1 cells stimulated by IL-5 after 48 hours of treatment, with an IC50 value of 0.091nM[4].
In vivo, seven days after intraperitoneal injection of a single dose of 200mg/kg Reslizumab, the number of eosinophils in the blood and the level of serum IL-5 in the ovalbumin (OVA)-treated mice were significantly reduced, without affecting the production of IL-13[5]. In OVA-sensitized guinea pig model, Reslizumab (1mg/kg) administered intraperitoneally 2 hours before the OVA challenge reduced eosinophilia, airway hyperreactivity, and bronchoconstriction[6].
References:
[1] Padilla Galo A, Labor M, Tiotiu A, et al. Impact of reslizumab on outcomes of severe asthmatic patients: current perspectives[J]. Patient Related Outcome Measures, 2018: 267-273.
[2] Hom S, Pisano M. Reslizumab (Cinqair): an interleukin-5 antagonist for severe asthma of the eosinophilic phenotype[J]. Pharmacy and Therapeutics, 2017, 42(9): 564.
[3] Xu Y, Yang L, Zhao T, et al. Multifunctional Gold Nanoclusters for a Lung Tissue Distribution Study of a Novel Anti-asthma Inhaled Antibody[J]. Analytical Chemistry, 2025, 97(36): 19635-19653.
[4] Liddament M, Husten J, Estephan T, et al. Higher binding affinity and in vitro potency of reslizumab for interleukin-5 compared with mepolizumab[J]. Allergy, Asthma & Immunology Research, 2018, 11(2): 291-298.
[5] Kageyama K, Kikuchi E, Hoshino N. Effect of anti-interleukin-5 antibody on development of vasculitis in an ovalbumin-induced eosinophilic vasculitis mouse model[J]. Frontiers in Pharmacology, 2025, 16: 1546785.
[6] Egan R W, Athwal D, Bodmer M W, et al. Effect of Sch 55700, a humanized monoclonal antibody to human interleukin-5, on eosinophilic responses and bronchial hyperreactivity[J]. Arzneimittelforschung, 1999, 49(09): 779-790.
Reslizumab是一种靶向IL-5分子的人源化IgG4/κ单克隆抗体,Kd值为81pM[1]。Reslizumab与嗜酸性粒细胞表面的IL-5受体α链结合,从而抑制嗜酸性粒细胞的增殖,并且Reslizumab可通过酶促蛋白水解代谢为小肽和氨基酸[2]。Reslizumab已广泛用于哮喘动物模型,以控制哮喘症状并改善肺功能[3]。
在体外,Reslizumab处理48小时后能显著抑制IL-5刺激的TF-1细胞增殖,IC50值为0.091nM[4]。
在体内,单次腹腔注射200mg/kg剂量的Reslizumab 7天后,卵清蛋白(OVA)处理小鼠血液中的嗜酸性粒细胞数量及血清IL-5水平显著降低,且不影响IL-13的产生[5]。在OVA致敏的豚鼠模型中,于OVA处理前2小时腹腔注射Reslizumab(1mg/kg),可减轻嗜酸性粒细胞增多、气道高反应性及支气管收缩[6]。
| Cell experiment [1]: | |
Cell lines | TF-1 cell |
Preparation Method | Add 50μl of TF-1 cell suspension (1×106) and 25μl of 0.045nM IL-5 to each well of a 96-well detection plate. Cultivate the cells in RPMI-1640 medium, supplemented with 10% fetal bovine serum, 2mM L-glutamine, 100U/ml penicillin-streptomycin, and 55µM β-mercaptoethanol, and pre-incubate at 37°C, 5% CO2 for 30-45 minutes. After pre-incubation, add 25μl of different concentrations of Reslizumab (0.001, 0.01, 0.1, 10nM) to each well. Place the plates in a humidified 37°C/5% CO2 incubator to cultivate for approximately 48 hours, and analyze the cell proliferation. |
Reaction Conditions | 0.001, 0.01, 0.1, 10nM; 48h |
Applications | Reslizumab treatment inhibited the proliferation of TF-1 in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6NCrSlc mice |
Preparation Method | Female C57BL/6NCrSlc mice (6 weeks old) were intraperitoneally injected with OVA (8μg per mouse) on days 0 and 14. Subsequently, based on the body weight on day 25, the mice were randomly stratified and grouped into groups of 5 or 7 mice each. On the day of the first OVA aerosol exposure (day 26), one injection of Reslizumab (200mg/kg) or the vehicle (normal saline) was given intraperitoneally (i.p.). From day 26 to day 32, the mice were placed in a plastic nebulization chamber (23×23×27cm) and inhaled 1% OVA (weight/volume) saline solution using a nebulizer for 1 hour each day. The negative control group (normal saline/vehicle) inhaled normal saline and received intravenous normal saline. The positive control group (1% OVA/vehicle) inhaled 1% OVA and received intravenous normal saline. On the third day of inhalation (day 28), 40µl of blood was drawn from the tail of the mice and plasma was separated for cytokine determination. |
Dosage form | 200mg/kg for once; i.p. |
Applications | Reslizumab treatment significantly suppressed the production of IL-5 in OVA-treated mice. |
References: | |
| Cas No. | 241473-69-8 | SDF | |
| 别名 | Sch 55700 | ||
| Canonical SMILES | [Reslizumab] | ||
| 分子式 | 分子量 | ||
| 溶解度 | Soluble in DMSO | 储存条件 | Store at 4°C,Do not freeze |
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