Ceftobiprole Medocaril Sodium

Storage temp: 4°C, sealed storage, away from moisture and light

Solubility: DMSO: 5 mg/mL (9.35 mM)

Form: Solid

Color: Off-white to Light Yellow

​Cell Experiment​​

​​DMSO:​​ 250 mg/mL (350.81 mM; Ultrasonic required)

Preparing Stock Solutions：

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Please prepare the stock solution in the appropriate solvent based on the product's solubility in different solvents. Once dissolved, aliquot the solution to avoid product inactivation caused by repeated freeze-thaw cycles.

​​Storage method and shelf life of the stock solution:​​ -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use within 6 months; when stored at -20°C, please use within 1 month.

Ceftobiprole has demonstrated in vitro activity against Gram-positive and Gram-negative bacteria. In a neutropenic murine thigh infection model, therapeutic efficacy is correlated with the time that the unbound plasma concentration of ceftobiprole exceeds the minimum inhibitory concentration (MIC) of S. aureus, S. pneumoniae, and Enterobacterales spp.

It is not active against Gram-negative bacteria producing extended-spectrum beta-lactamases (ESBLs) from the TEM, SHV, or CTX-M families, serine carbapenemases (such as KPC), class B metallo-beta-lactamases, class C (AmpC cephalosporinases) if expressed at high levels, and Ambler class D beta-lactamases including carbapenemases.

Ceftobiprole is not indicated for use in patients with ventilator-associated bacterial pneumonia (VABP) - in clinical trials, a statistically significant increase in mortality was seen in patients with VABP treated with ceftobiprole medocaril as compared to comparator-treated patients.

Ceftobiprole, the active moiety of ceftobiprole medocaril, exhibits its bactericidal activity by inhibition of bacterial cell wall synthesis. This activity is mediated through binding to essential penicillin-binding proteins (PBPs) and inhibiting their transpeptidase activity, which is essential for the synthesis of the peptidoglycan layer of the bacterial cell wall. Ceftobiprole has demonstrated in vitro activity against both Gram-positive and Gram-negative bacteria. In Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA), Ceftobiprole binds to PBP2a. Ceftobiprole also binds to PBP2b in Streptococcus pneumoniae (penicillin-intermediate), PBP2x in S. pneumoniae (penicillin resistant), and to PBP5 in Enterococcus faecalis.