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Avibactam sodium

CAS No. : 1192491-61-4

MCE 站：Avibactam sodium

产品活性：Avibactam sodium (NXL-104) 是一种共价，可逆的非β-内酰胺 β-内酰胺酶抑制剂 (β-lactamase) 抑制剂，抑制 β-lactamase TEM-1 和 CTX-M-15，IC₅₀ 分别为 8 nM 和 5 nM。

研究领域：Anti-infection

作用靶点：Bacterial  |  Antibiotic

In Vitro: Avibactam (NXL104) sodium is a molecule with little antibacterial activity, that inhibits class A and C β-lactamases. Avibactam inactivates most important β-lactamases except metallo types and Acinetobacter OXA carbapenemases.

In Vivo: Avibactam sodium (NXL-104) displays a slow return of activity with an off-rate of 0.045±0.022 min^-1, which converts to a residence time half-life (t_t1/2) of 16±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 t_1/2 values of >1 or >7 d for Avibactam inhibition of TEM-1. Avibactam is a new promising β-lactamase inhibitor, to overcome resistance caused by β-lactamases. 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 GR20263 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 GR20263 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.

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