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Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Avibactam sodium (NXL-104) is a reversible β-lactamase inhibitor (IC50: 8/80/38 nM, for TEM-1/P99/KPC-2 β-lactamases).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 35.00 | |
5 mg | In stock | $ 56.00 | |
10 mg | In stock | $ 77.00 | |
25 mg | In stock | $ 93.00 | |
50 mg | In stock | $ 127.00 | |
100 mg | In stock | $ 187.00 | |
200 mg | In stock | $ 257.00 | |
500 mg | In stock | $ 435.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 56.00 |
Description | Avibactam sodium (NXL-104) is a reversible β-lactamase inhibitor (IC50: 8/80/38 nM, for TEM-1/P99/KPC-2 β-lactamases). |
Targets&IC50 | TEM-1:8 nM, P99:80 nM, KPC-2:38 nM |
In vitro | Avibactam (NXL104) sodium has little antibacterial activity and inhibits class A and C β-lactamases. Except for Metallo types and Acinetobacter OXA carbapenemases, Avibactam inactivates the most of important β-lactamases[2]. |
In vivo | Avibactam 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. Avibactam has slow deacylation through hydrolysis or reversibility, and this is in contrast to previously reported extremely long t1/2 values of >1 or >7 d for Avibactam inhibition of TEM-1[1]. 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 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 L/kg (SD, 0.14 L/kg) and 1.18 liters/kg (SD, 0.34 L/kg), respectively. |
Kinase Assay | 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 is diluted with 180 μL assay buffer to restore the original enzyme concentration. After two UFC treatments, the amount of free Avibactam is quantified by LC/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 a non-UFC-treated enzyme, and loss is found to be <5%[1]. |
Cell Research | Avibactam is prepared in sterile water[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]. |
Animal Research | Avibactam is reconstituted in sterile water to a stock solution of 5,120 mg/L and the 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) and to cover a wide range of doses of each compound. |
Synonyms | AVE-1330A, NXL-104 |
Molecular Weight | 287.22 |
Formula | C7H10N3NaO6S |
CAS No. | 1192491-61-4 |
keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 53 mg/mL (184.5 mM)
H2O: 52 mg/mL (181 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Avibactam sodium 1192491-61-4 Microbiology/Virology Antibacterial Antibiotic inhibit antibacterial Avibactam AVE-1330A NXL 104 Bacterial TEM-1 β-lactamase Inhibitor Klebsiella pneumonia Pseudomonas aeruginosa NXL-104 NXL104 inhibitor