Ceftolozane Sulfate is a broad-spectrum cephalosporin with bactericidal activity.
Ceftolozane Sulfate is the sulfate salt of Ceftolozane, a broad-spectrum, fifth-generation cephalosporin with bactericidal activity. 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 |
