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Avibactam sodium

Catalog No. T4201   CAS 1192491-61-4
Synonyms: AVE-1330A, NXL-104

Avibactam sodium (NXL-104) is a reversible β-lactamase inhibitor (IC50: 8/80/38 nM, for TEM-1/P99/KPC-2 β-lactamases).

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Avibactam sodium Chemical Structure
Avibactam sodium, CAS 1192491-61-4
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
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Purity: 100%
Purity: 99.95%
Purity: 99.56%
Purity: 99.16%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

keep away from direct sunlight

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 53 mg/mL (184.5 mM)

H2O: 52 mg/mL (181 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Inhibitor Library Antibiotics Library Drug-induced Liver Injury (DILI) Compound Library Anti-Infection Compound Library Bioactive Compound Library Beta-Lactam Compound Library Nonsteroidal Anti-Inflammatory Compound Library Anti-Bacterial Compound Library Drug Repurposing Compound Library

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Keywords

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

 

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