Ceftaroline fosamil
(Synonyms: 头孢洛林酯; TAK-599; PPI0903) 目录号 : GC35646
Ceftaroline fosamil是具有生物活性的ceftaroline的水溶性前体药，具有广谱抗菌活性。
Cas No.:400827-46-5
Sample solution is provided at 25 µL, 10mM.
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Ceftaroline fosamil is a water-soluble prodrug of the bioactive ceftaroline with the broad-spectrum antibacterial activity [1]. The bactericidal action of Ceftaroline fosamil is mediated through binding to PBPs on bacterial cell walls, leading to irreversible inhibition of cell-wall synthesis[2]. Ceftaroline fosamil has been widely used to kill drug-resistant Gram-positive and Gram-negative bacteria, as well as to treat experimental bacteraemia in animal models[3].
In vitro, Ceftaroline fosamil treatment for 24 hours significantly inhibited SARS-CoV-2 replication in Calu-3 cells with an EC50 value of 1.25µM[4].
In vivo, Ceftaroline fosamil treatment via intramuscular injection at a dose of 60mg/kg/day for 7 days significantly reduced the density of methicillin-resistant Staphylococcus aureus (MRSA) in the rabbit prosthetic joint infection model[5]. Ceftaroline fosamil (40mg/kg) administered intramuscularly every 8 hours for 3 days reduced the activity of MRSA in a rat model of endocarditis[6]. In a rabbit model of acute MRSA-infected osteomyelitis, treatment with Ceftaroline fosamil (10mg/kg) twice intravenously for 4 days significantly reduced bacterial density in synovial fluid, bone marrow, and bone[7].
References:
[1] Ye L, Zhang J, Xiao W, et al. Efficacy and mechanism of actions of natural antimicrobial drugs[J]. Pharmacology & Therapeutics, 2020, 216: 107671.
[2] Poon H, Chang M H, Fung H B. Ceftaroline fosamil: a cephalosporin with activity against methicillin-resistant Staphylococcus aureus[J]. Clinical therapeutics, 2012, 34(4): 743-765.
[3] García P, Moscoso M, Fernández M C, et al. Comparison of the in vivo efficacy of ceftaroline fosamil, vancomycin and daptomycin in a murine model of methicillin-resistant Staphylococcus aureus bacteraemia[J]. International Journal of Antimicrobial Agents, 2023, 62(1): 106836.
[4] Delgado C, Nogara P A, Miranda M D, et al. In Silico and In Vitro Studies of the Approved Antibiotic Ceftaroline Fosamil and Its Metabolites as Inhibitors of SARS-CoV-2 Replication[J]. Viruses, 2025, 17(4): 491.
[5] Gatin L, Saleh-Mghir A, Tasse J, et al. Ceftaroline-Fosamil efficacy against methicillin-resistant Staphylococcus aureus in a rabbit prosthetic joint infection model[J]. Antimicrobial agents and chemotherapy, 2014, 58(11): 6496-6500.
[6] Singh K V, Tran T T, Nannini E C, et al. Efficacy of ceftaroline against methicillin-susceptible Staphylococcus aureus exhibiting the cefazolin high-inoculum effect in a rat model of endocarditis[J]. Antimicrobial Agents and Chemotherapy, 2017, 61(7): 10.1128/aac. 00324-17.
[7] Jacqueline C, Amador G, Caillon J, et al. Efficacy of the new cephalosporin ceftaroline in the treatment of experimental methicillin-resistant Staphylococcus aureus acute osteomyelitis[J]. Journal of antimicrobial chemotherapy, 2010, 65(8): 1749-1752.
Ceftaroline fosamil是具有生物活性的ceftaroline的水溶性前体药，具有广谱抗菌活性[1]。Ceftaroline fosamil的杀菌作用是通过与细菌细胞壁上的PBPs结合，从而不可逆地抑制细胞壁合成[2]。Ceftaroline fosamil已被广泛用于杀灭耐药革兰氏阳性和革兰氏阴性细菌，并在动物模型中用于治疗实验性菌血症[3]。
在体外，用Ceftaroline fosamil处理Calu-3细胞24小时可显著抑制SARS-CoV-2病毒复制，EC50值为1.25µM[4]。
在体内，以60mg/kg/day的剂量肌肉注射Ceftaroline fosamil治疗7天，可显著降低兔人工关节感染模型中methicillin-resistant Staphylococcus aureus (MRSA)的密度[5]。在大鼠心内膜炎模型中，以40mg/kg的剂量每8小时肌肉注射一次Ceftaroline fosamil，治疗3天，可降低MRSA的活性[6]。在兔急性MRSA感染性骨髓炎模型中，以10mg/kg的剂量静脉注射Ceftaroline fosamil，每日两次，治疗4天，可显著降低滑液、骨髓和骨骼中的细菌密度[7]。
| Cell experiment [1]: | |
Cell lines | Calu-3 cells |
Preparation Method | Calu-3 cells were cultured in high-glucose Dulbecco's modified Eagle medium (DMEM) supplemented with 1% penicillin/streptomycin, HEPES buffer, and 10% fetal bovine serum (FBS). The culture conditions were 37℃ and 5% CO2 in a humid environment. The cells were seeded in 96-well plates with a cell density of 1.5×104 cells/well and cultured in an incubator at 37 °C with 5% CO₂. Cells were infected with SARS-CoV-2 at a multiplicity of infection (MOI) of 0.01 and cultured for 1 hour at 37℃ in 5% CO2 atmosphere. Subsequently, the cells were treated with different concentrations of Ceftaroline fosamil (0.1, 0.316, 1, 3.16, and 10µM) for 24h, and 20µl of the supernatant was collected for viral titer determination. |
Reaction Conditions | 0.1, 0.316, 1, 3.16, and 10µM; 24h |
Applications | Ceftaroline fosamil treatment inhibited viral replication of SARS-CoV-2 in SARS-CoV-2 in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | New Zealand White rabbits |
Preparation Method | New Zealand white rabbits (2.5-3kg) were housed individually in cages and maintained on a natural light-dark cycle. Each rabbit underwent a partial right knee replacement with a tibial prosthesis. Immediately after surgery, 5×10⁷ CFU of MRSA was inoculated into the rabbits in a 0.5ml volume of phosphate buffer near the knee joint where the prosthesis was located. On day 7 post-infection, rabbits were started to receive Ceftaroline fosamil (60mg/kg/day; s.c.), for 7 days. The control group received no treatment. Rabbit tibia tissues were collected for analysis. |
Dosage form | 60mg/kg/day for 7 days; s.c. |
Applications | Ceftaroline fosamil treatment significantly reduced the density of MRSA in the tibia of rabbit. |
References: | |
| Cas No. | 400827-46-5 | SDF | |
| 别名 | 头孢洛林酯; TAK-599; PPI0903 | ||
| Canonical SMILES | O=C1[C@@H](NC(/C(C2=NSC(NP(O)(O)=O)=N2)=N\OCC)=O)[C@@]3([H])SCC(SC4=NC(C5=CC=[N+](C)C=C5)=CS4)=C(C(O)=O)N13.CC([O-])=O | ||
| 分子式 | C24H25N8O10PS4 | 分子量 | 744.74 |
| 溶解度 | DMSO: 30 mg/mL (40.28 mM and warming) | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3428 mL | 6.7138 mL | 13.4275 mL |
| 5 mM | 268.6 μL | 1.3428 mL | 2.6855 mL |
| 10 mM | 134.3 μL | 671.4 μL | 1.3428 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
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