Ceftolozane Sulfate is a broad-spectrum, fifth-generation cephalosporin with bactericidal activity belonging to the β-lactam group of antibiotics. It can be used in biopharma research for impurity profiling and chemical stability testing. It can be used for impurity profiling, penicillin binding protein (PBP) studies and infection models. It was approved by the FDA in 2014 (Cubist Pharmaceuticals) in combination with tazobactam, a β-lactamase inhibitor.
Ceftolozane Sulfate is soluble in DMSO.
We also offer:
- Ceftolozane Sulfate (stabilized with arginine) (C261)
| 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. Ceftolozane is a potent PBP3 inhibitor and has a higher affinity for PBP1b compared with other β-lactam agents. 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 | Ceftolozane Sulfate is 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 µg/ml. It was highly stable against AmpC β-lactamase, the main resistance mechanism for cephalosporins (Takeda et al, 2007). |
| Molecular Formula | C23H31N12O8S2 ∙ HSO4 |
| References |
Cho JC, Fiorenza MA, Estrada SJ (2015) Ceftolozane/Tazobactam: A Novel Cephalosporin/β-Lactamase Inhibitor Combination. Pharmacother. 35(7):701-715 PMID 26133315 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 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 |
