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Avibactam (NXL-104) free acid is a covalent and reversible inhibitor of non-尾-lactam 尾-lactamase (IC50s: 8 nM and 5 nM for 尾-lactamase TEM-1 and CTX-M-15).
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Avibactam inhibits class A and C 尾-lactamases. Avibactam inactivates the most important 尾-lactamases except metallo types and Acinetobacter OXA carbapenemases [2].
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Avibactam sodium displays a slow return of activity with an off-rate of 0.045卤0.022/min, which converts to a residence time half-life (tt1/2) of 16卤8 min. The measured off-rate for Avibactam suggests that slow deacylation through hydrolysis or reversibility is occurring, and it is in contrast to previously reported extremely long t1/2 values of >1 or >7 d for Avibactam inhibition of TEM-1 [1]. Mice are infected with ca.106 CFU of Pseudomonas aeruginosa intramuscularly into the thigh or intranasally to cause pneumonia and are given 8 different (single) subcutaneous doses of Ceftazidime and Avibactam in various combined concentrations, ranging from 1 to 128 mg/kg of body weight in 2-fold increases. The mean estimated half-life in plasma of Ceftazidime in the terminal phase is 0.28 h (SD, 0.02 h), and that of Avibactam is 0.24 h (SD, 0.04 h). Volumes of distribution are 0.80 liters/kg (SD, 0.14 liters/kg) and 1.18 liters/kg (SD, 0.34 liters/kg), respectively [3].
Cas No.
1192500-31-4
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C7H11N3O6S
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265.24
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NXL-104 free acid
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(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20掳C for 3 years
In solvent: -80掳C for 2 years