Avibactam
Catalog No.: GC14602Purity:>98.00%Synonyms: NXL-104 free acid
A β-lactamase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1192500-31-4
10mM (in 1mL DMSO)In Stock
$55.00
1
2mgIn Stock
$35.00
1
5mgIn Stock
$46.00
1
10mgIn Stock
$67.00
1
50mgIn Stock
$154.00
1
100mgIn Stock
$231.00
1
200mgIn Stock
$350.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $55.00 | In Stock | 1 | |
| 2mg | $35.00 | In Stock | 1 | |
| 5mg | $46.00 | In Stock | 1 | |
| 10mg | $67.00 | In Stock | 1 | |
| 50mg | $154.00 | In Stock | 1 | |
| 100mg | $231.00 | In Stock | 1 | |
| 200mg | $350.00 | In Stock | 1 |
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Citations
3 publicationsPublications from researchers using this productDescription
Avibactam free acid (NXL-104 free acid) is a covalent, reversible non-β-lactam β-lactamase inhibitor, inhibits β-lactamase TEM-1 and CTX-M-15 with IC50 of 8 nM and 5 nM, respectively.
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].
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].
References:
[1]. Ehmann DE, et al. Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8.
[2]. Livermore DM, et al. Characterization of β-lactamase and porin mutants of Enterobacteriaceae selected with ceftaroline + avibactam (NXL104). J Antimicrob Chemother. 2012 Jun;67(6):1354-8.
[3]. Berkhout J, et al. Pharmacokinetics and penetration of ceftazidime and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrob Agents Chemother. 2015 Apr;59(4):2299-304.
Protocol
Cell experiment: | 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]. |
Animal experiment: | 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. |
References: [1]. Ehmann DE, et al. Avibactam is a covalent, reversible, non-β-lactam β-lactamase inhibitor. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8. | |
Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
1192500-31-4
Synonyms
NXL-104 free acid
Chemical Name
(2R,5S)-7-oxo-6-(sulfooxy)-1,6-diazabicyclo[3.2.1]octane-2-carbimidic acid
SMILES
N=C(O)[C@@]1([H])CC[C@@](N2OS(O)(=O)=O)([H])CN1C2=O
Molecular Formula
C7H11N3O6S
Molecular Weight
265.24
Solubility
DMSO : 125 mg/mL (471.27 mM; Need ultrasonic)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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