Cefiderocol (S-649266)
(Synonyms: 头孢地尔; S-649266) 目录号 : GC32079
Cefiderocol是一种新型铁载体头孢菌素，对革兰氏阴性菌和非发酵革兰氏阴性菌具有较强的体外活性。
Cas No.:1225208-94-5
Sample solution is provided at 25 µL, 10mM.
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Cefiderocol is a new type of iron carrier cephalosporin with strong in vitro activity against Gram-negative bacteria and non-fermented Gram-negative bacteria[1-3].
Cefiderocol(10/40/70 mg/L;3 days) dampens LPS-stimulated production of pro-inflammatory cytokines[4]. The absence of iron transporters PiuA in Pseudomonas aeruginosa or CirA and Fiu in Escherichia coli resulted in a 16-fold increase in cefiderocol MIC, suggesting that these iron transporters contribute to cefiderocol penetration through the outer membrane[5].
Administering cefiderocol 2 g every 8 h as a 3-h infusion for 4 days achieved a greater than 3 log10 reduction in cells of carbapenem-resistant isolates of P. aeruginosa, A. baumannii, and K. pneumoniae in rat lung infection[6]. The pharmacodynamics of cefiderocol in the thigh infection model of neutropenia mice showed a sigmoid dose-response curve, and the bactericidal effect was better with the increase of dose[7].
References:
[1]. Choi JJ, McCarthy MW. Cefiderocol: a novel siderophore cephalosporin. Expert Opin Investig Drugs. 2018 Feb;27(2):193-197. doi: 10.1080/13543784.2018.1426745. Epub 2018 Jan 24. PMID: 29318906.
[2]. Soriano MC, Montufar J,et,al. Cefiderocol. Rev Esp Quimioter. 2022 Apr;35 Suppl 1(Suppl 1):31-34. doi: 10.37201/req/s01.07.2022. Epub 2022 Apr 22. PMID: 35488822; PMCID: PMC9106201.
[3]. GijÓn Cordero D, Castillo-Polo JA, et,al. Antibacterial spectrum of cefiderocol. Rev Esp Quimioter. 2022 Sep;35 Suppl 2(Suppl 2):20-27. doi: 10.37201/req/s02.03.2022. Epub 2022 Oct 4. PMID: 36193981; PMCID: PMC9632062.
[4]. Hildebrand D, BÖhringer J, et,al. Cefiderocol Protects against Cytokine- and Endotoxin-Induced Disruption of Vascular Endothelial Cell Integrity in an In Vitro Experimental Model. Antibiotics (Basel). 2022 Apr 26;11(5):581. doi: 10.3390/antibiotics11050581. PMID: 35625225; PMCID: PMC9137736.
[5]. Ito A, Sato T, et,al. In Vitro Antibacterial Properties of Cefiderocol, a Novel Siderophore Cephalosporin, against Gram-Negative Bacteria. Antimicrob Agents Chemother. 2017 Dec 21;62(1):e01454-17. doi: 10.1128/AAC.01454-17. PMID: 29061741; PMCID: PMC5740388.
[6]. Matsumoto S, Singley CM, et,al. Efficacy of Cefiderocol against Carbapenem-Resistant Gram-Negative Bacilli in Immunocompetent-Rat Respiratory Tract Infection Models Recreating Human Plasma Pharmacokinetics. Antimicrob Agents Chemother. 2017 Aug 24;61(9):e00700-17. doi: 10.1128/AAC.00700-17. PMID: 28630178; PMCID: PMC5571323.
[7]. Ghazi IM, Monogue ML, et,al. Pharmacodynamics of cefiderocol, a novel siderophore cephalosporin, in a Pseudomonas aeruginosa neutropenic murine thigh model. Int J Antimicrob Agents. 2018 Feb;51(2):206-212. doi: 10.1016/j.ijantimicag.2017.10.008. Epub 2017 Oct 27. PMID: 29111435.
Cefiderocol是一种新型铁载体头孢菌素,对革兰氏阴性菌和非发酵革兰氏阴性菌具有较强的体外活性[1-3]。
Cefiderocol(10/40/70 mg/L；3 天）抑制 LPS 刺激的促炎细胞因子的产生[4]。铜绿假单胞菌中铁转运体 PiuA 或大肠杆菌中 CirA 和 Fiu 的缺失导致头孢地尔考 MIC 增加 16 倍,表明这些铁转运体有助于头孢地尔考穿过外膜[5]。
<p >每 8 小时给予 2 克头孢地尔考 3 小时输注 4 天,使大鼠肺部感染的铜绿假单胞菌、鲍曼不动杆菌和肺炎克雷伯菌的碳青霉烯类耐药菌株的细胞减少了 3 log10 以上[6 ].头孢地尔考在白细胞减少小鼠大腿感染模型中的药效学呈S型剂量-反应曲线,随着剂量的增加杀菌效果更好[7]。
| Cell experiment [1]: | |
|
Cell lines |
Peripheral blood mononuclear cells (PBMCs) |
|
Preparation Method |
Cells were stimulated with 100 ng/mL LPS with or without cefiderocol (10 mg/L, 40 mg/L, 70 mg/L) for 3 days |
|
Reaction Conditions |
10/40/70 mg/L;3 days |
|
Applications |
Higher concentrations of cefiderocol inhibit the production of lipopolysaccharide-stimulated proinflammatory cytokines. |
| Animal experiment [2]: | |
|
Animal models |
Pathogen-free male Sprague-Dawley rats |
|
Preparation Method |
Inoculants of 0.1 ml(Pseudomonas aeruginosa) or 0.2 ml(Pseudomonas baumannii or Klebsiella pneumoniae) were injected into the lungs of rats to induce respiratory infection, The infected rats were given cefiderocol subcutaneously. |
|
Dosage form |
2 g every 8 h as a 3-h infusion for 4 days |
|
Applications |
Administering cefiderocol 2 g every 8 h as a 3-h infusion for 4 days achieved a greater than 3 log10 reduction in cells of carbapenem-resistant isolates of P. aeruginosa, A. baumannii, and K. pneumoniae in rat lung infection. |
|
References: [1]. Hildebrand D, BÖhringer J, et,al. Cefiderocol Protects against Cytokine- and Endotoxin-Induced Disruption of Vascular Endothelial Cell Integrity in an In Vitro Experimental Model. Antibiotics (Basel). 2022 Apr 26;11(5):581. doi: 10.3390/antibiotics11050581. PMID: 35625225; PMCID: PMC9137736. |
|
| Cas No. | 1225208-94-5 | SDF | |
| 别名 | 头孢地尔; S-649266 | ||
| Canonical SMILES | O=C(C(N12)=C(C[N+]3(CCNC(C4=CC=C(O)C(O)=C4Cl)=O)CCCC3)CS[C@]2([H])[C@H](NC(/C(C5=CSC(N)=N5)=N\OC(C)(C(O)=O)C)=O)C1=O)[O-] | ||
| 分子式 | C30H34ClN7O10S2 | 分子量 | 752.21 |
| 溶解度 | DMSO : 50 mg/mL (66.47 mM) | 储存条件 | Store at -20°C, stored under nitrogen,unstable in solution, ready to use. |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.3294 mL | 6.6471 mL | 13.2942 mL |
| 5 mM | 0.2659 mL | 1.3294 mL | 2.6588 mL |
| 10 mM | 0.1329 mL | 0.6647 mL | 1.3294 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: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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