|(6R,7R)-7-((Z)-2-(2-氨基噻唑-4-基)-2-((2-羧丙基-2-基)氧基)亚胺基)乙酰胺基)-3-((1-(2-(2-氯-3,4-二羟基苯甲酰胺基)乙基)吡咯烷-1-ium-1-基)甲基)-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸盐|CsnPharm

CAS No.: 1225208-94-5

Cefiderocol/头孢地尔 Catalog No. CSN21224

Synonyms: S-649266;GSK-2696266D;S-649266D

Cefiderocol is a novel siderophore cephalosporin which has a potent activity against a broad range of aerobic Gram-negative bacterial species with MIC50s of 2 μg/mL or less.

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实验方案

技术信息

生物活性

描述Cefiderocol (CFDC; S-649266), a novel parenteral siderophore cephalosporin conjugated with a catechol moiety, has a characteristic antibacterial spectrum with a potent activity against a broad range of aerobic Gram-negative bacterial species, including carbapenem-resistant strains of Enterobacteriaceae and nonfermenting bacteria such as Pseudomonas aeruginosa and Acinetobacter baumannii. Cefiderocol has affinity mainly for penicillin-binding protein 3 (PBP3) of Enterobacteriaceae and nonfermenting bacteria similar to that of ceftazidime^[1]. The principal antibacterial/bactericidal activity of cefiderocol occurs by inhibition of Gram-negative bacterial cell wall synthesis by binding to penicillin binding proteins; however, it is unique in that it enters the bacterial periplasmic space as a result of its siderophore-like property and has enhanced stability to β-lactamases. Cefiderocol is also more potent than both ceftazidime-avibactam and meropenem versus Acinetobacter baumannii, including meropenem non-susceptible and multidrug-resistant (MDR) isolates^[2]. Furthermore, cefiderocol has demonstrated structural stability against hydrolysis by both serine- and metallo-β-lactamases, including clinically relevant carbapenemases such as Klebsiella pneumoniae carbapenemase, oxacillin carbapenemase-48, and New Delhi metallo-β-lactamase^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02714595	Healthcare-associated Pneumoni... more >>a (HCAP) Bloodstream Infections (BSI) Hospital Acquired Pneumonia (HAP) Complicated Urinary Tract Infection (cUTI) Sepsis Ventilator Associated Pneumonia (VAP) Collapse <<	Phase 3	Recruiting	May 19, 2019	-
NCT02321800	Urinary Tract Infections	Phase 2	Completed	-	-
NCT03032380	Healthcare-associated Pneumoni... more >>a (HCAP) Hospital Acquired Pneumonia (HAP) Ventilator Associated Pneumonia (VAP) Collapse <<	Phase 3	Recruiting	February 1, 2019	-

参考文献

[1] Ito A, Sato T, Ota M, et al. In Vitro Antibacterial Properties of Cefiderocol, a Novel Siderophore Cephalosporin, against Gram-Negative Bacteria. Antimicrob Agents Chemother. 2017;62(1):e01454-17.
[2] Zhanel GG, Golden AR, Zelenitsky S, et al. Cefiderocol: A Siderophore Cephalosporin with Activity Against Carbapenem-Resistant and Multidrug-Resistant Gram-Negative Bacilli. Drugs. 2019;79(3):271-289
[3] Sato T, Yamawaki K. Cefiderocol: Discovery, Chemistry, and In Vivo Profiles of a Novel Siderophore Cephalosporin. Clin Infect Dis. 2019;69(Suppl 7):S538-S543

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.3294 mL
- 6.6470 mL
- 13.2941 mL
- 5 mM
- 0.2659 mL
- 1.3294 mL
- 2.6588 mL
- 10 mM
- 0.1329 mL
- 0.6647 mL
- 1.3294 mL

技术信息

CAS号

1225208-94-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H34ClN7O10S2

运输

蓝冰

分子量

752.21

别名

S-649266;GSK-2696266D;S-649266D;Fetroja;头孢地尔

溶解度

DMSO	50.0 mg/mL (66.5 mM) warming

动物实验配方

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