1. Anti-infection
  2. Bacterial
    Antibiotic
  3. Avibactam free acid

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

Cat. No.: HY-14879 Purity: >98.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

Avibactam free acid Chemical Structure

Avibactam free acid Chemical Structure

CAS No. : 1192500-31-4

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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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    Description

    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].

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

    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].

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

    Clinical Trial
    Molecular Weight

    265.24

    Formula

    C₇H₁₁N₃O₆S

    CAS No.

    1192500-31-4

    SMILES

    O=S(ON1[[email protected]]2([H])CC[[email protected]@H](C(N)=O)[[email protected]@](C2)C1=O)(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    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
    [3]

    Mice[3]
    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.

    References
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    Keywords:

    AvibactamNXL-104NXL104NXL 104BacterialAntibioticInhibitorinhibitorinhibit

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