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  3. Avibactam sodium

Avibactam sodium (Synonyms: NXL-104)

Cat. No.: HY-14879A Purity: 99.75%
Handling Instructions

Avibactam sodium (NXL-104) 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 sodium Chemical Structure

Avibactam sodium Chemical Structure

CAS No. : 1192491-61-4

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of Avibactam sodium:

Top Publications Citing Use of Products

    Avibactam sodium 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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Avibactam sodium (NXL-104) 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) 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[2].

    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 (tt1/2) 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 t1/2 values of >1 or >7 d for Avibactam 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 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[3].

    Clinical Trial
    Molecular Weight

    287.23

    Formula

    C₇H₁₀N₃NaO₆S

    CAS No.

    1192491-61-4

    SMILES

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

    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
    Solvent & Solubility
    In Vitro: 

    H2O : 50 mg/mL (174.08 mM; Need ultrasonic)

    DMSO : ≥ 30 mg/mL (104.45 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.4815 mL 17.4077 mL 34.8153 mL
    5 mM 0.6963 mL 3.4815 mL 6.9631 mL
    10 mM 0.3482 mL 1.7408 mL 3.4815 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    In a 200 μL reaction volume, 1 μM TEM-1 is incubated with and without 5 μM Avibactam for 5 min at 37°C and subjected to two ultrafiltration cartridge (UFC) steps to remove excess inhibitor (Ultrafree-0.5 with Biomax membrane, 5-kDa cutoff). Centrifugation at 10,600× g for 8 min is performed at 4°C. After each ultrafiltration step, 20 μL retentate are diluted with 180 μL assay buffer to restore the original enzyme concentration. After two UFC treatments, the amount of free Avibactam is quantified by liquid chromotography/MS/MS and found to be <5% of the original concentration. Loss of protein during UFC is assessed by measuring TEM-1 activity (on 4,000-fold dilution) in the acyl-enzyme sample compare with non-UFC-treated enzyme, and loss is found to be <5%[1].

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

    Cell Assay
    [2]

    Cells (~109 cfu) from overnight broth culture are spread on Mueller-Hinton agar supplemented with either (i) Ceftaroline plus Avibactam (1 or 4 mg/L) at 1-16× the MICs or (ii) Ceftaroline at 1 or 4 mg/L plus Avibactam 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 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 GR20263 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 (GR20263 and Avibactam) 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

    Purity: 99.75%

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    Keywords:

    AvibactamNXL-104NXL104NXL 104BacterialInhibitorinhibitorinhibit

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