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  3. Avibactam free acid

Avibactam free acid (Synonyms: NXL-104 free acid)

目录号: HY-14879 纯度: >98.0%

Avibactam free acid (NXL-104 free acid) 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-1CTX-M-15IC50 分别为 8 nM 和 5 nM。

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Avibactam free acid Chemical Structure

Avibactam free acid Chemical Structure

CAS No. : 1192500-31-4

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Avibactam free acid 的其他形式现货产品:

Other Forms of Avibactam free acid:

Top Publications Citing Use of Products

    Avibactam free acid purchased from MCE. Usage Cited in: J Antimicrob Chemother. 2017 Jul 1;72(7):1930-1936.

    Total β-lactamase activity for bacterial lysates is measured using the chromogenic substrate nitrocefin, with or without Avibactam at 4 mg/L. (b) GR20263 hydrolysis activity of different bacterial lysates is determined with or without Avibactam at 4 mg/L.
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    • 实验参考方法

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    • 参考文献


    Avibactam free acid (NXL-104 free acid) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.

    IC50 & Target

    IC50: 8 nM (TEM-1), 5 nM (CTX-M-15)[1]

    In Vitro

    Avibactam (NXL104) is a molecule with little antibacterial activity, that inhibits class A and C β-lactamases. Avibactam (NXL104) inactivates most important β-lactamases except metallo types and Acinetobacter OXA carbapenemases[2].

    In Vivo

    Avibactam (NXL104) sodium 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 (tt1/2) of 16±8 min. The measured off-rate for Avibactam (NXL104) 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 (NXL104) inhibition of TEM-1[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 Ceftazidime and Avibactam (NXL104) 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].

    Clinical Trial
    Molecular Weight




    CAS No.







    Room temperature in continental US; may vary elsewhere.

    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Cell Assay

    Cells (~109 cfu) from overnight broth culture are spread on Mueller-Hinton agar supplemented with either (i) Ceftaroline plus Avibactam (NXL104) (1 or 4 mg/L) at 1-16× the MICs or (ii) Ceftaroline at 1 or 4 mg/L plus Avibactam (NXL104) at 1-8× the concentration needed to reduce the Ceftaroline MIC to 1 or 4 mg/L. Colonies are counted after overnight incubation and representatives are retained[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration

    Avibactam (NXL104) is reconstituted in sterile water to a stock solution of 5,120 mg/L and further solution is prepared in Mueller-Hinton broth. Outbred female CD-1 mice, 7 to 8 weeks old and weighing 20 to 25 g, are used in the experiments. Eight dose combinations are used. For the thigh-infected animals, the combinations of Ceftazidime and Avibactam are 16/4, 8/1, 64/32, and 2/128 mg/kg. For the lung-infected mice, combinations of 32/16, 4/2, 128/8, and 1/64 mg/kg of the respective constituents are used. These combinations are chosen in order to detect possible pharmacokinetic interactions between the two compounds (Ceftazidime and Avibactam (NXL104)) and to cover a wide range of doses of each compound.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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    The dilution calculator equation

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    × = ×
    C1   V1   C2   V2


    AvibactamNXL-104NXL104NXL 104BacterialAntibioticInhibitorinhibitorinhibit


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