Ceftolozane Sulfate is a broad-spectrum cephalosporin with bactericidal activity.
Ceftolozane Sulfate is the sulfate salt of Ceftolozane, a broad-spectrum, fifth-generation cephalosporin. It can be used in biopharma research for impurity profiling and chemical stability testing. It can also be used for PBP binding profiles and infection models.
| Mechanism of Action | Ceftolozane Sulfate is a 3'-aminopyrazolium cephalosporin. Cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid-encoded β-lactamases such as AmpC β-lactamase. |
| Spectrum | Effective against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa and E. coli. |
| Microbiology Applications | In a study of P. aeruginosa using murine pulmonary, urinary tract, and burn wound models of infection, Ceftolozane's efficacy was comparable or superior to ceftazidime and imipenem. The MIC that inhibited 90% of isolates was 1 ug/ml. It was highly stable against AmpC beta-lactamase, the main resistance mechanism for cephalosporins (Takeda et al, 2007). |
| Molecular Formula | C23H31N12O8S2 ∙ HSO4 |
| References | Takeda S, Nakai T, Wakai Y, Ikeda F, and Hatano K (2007) In vitro and in vivo activities of a new cephalosporin, FR264205, against Pseudomonas aeruginosa. Antimicrob. Agents. Chemother. 51(3):826-830 PMID 17145788 Toda A et al (2008) Synthesis and SAR of novel parenteral anti-pseudomonal cephalosporins: Discovery of FR264205. Bioorg. Med. Chem. Lett. 18(17):4849-4852 Melchers MJB, van Mil ACH, Mouton JW (2015) In vitro activity of Ceftolozane alone and in combination with Tazobactam against extended-spectrum-β-lactamase-harboring Enterobacteriaceae. Antimicrob. Agents Chemother. 59 (8):4521-4525 |
