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Avibactam free acid

Catalog No. T10422   CAS 1192500-31-4
Synonyms: NXL-104 free acid

Avibactam (NXL-104) free acid is a covalent and reversible inhibitor of non-β-lactam β-lactamase (IC50s: 8 nM and 5 nM for β-lactamase TEM-1 and CTX-M-15).

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Avibactam free acid Chemical Structure
Avibactam free acid, CAS 1192500-31-4
Pack Size Availability Price/USD Quantity
2 mg 5 days $ 37.00
5 mg 5 days $ 57.00
1 mL * 10 mM (in DMSO) 5 days $ 64.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Avibactam (NXL-104) free acid is a covalent and reversible inhibitor of non-β-lactam β-lactamase (IC50s: 8 nM and 5 nM for β-lactamase TEM-1 and CTX-M-15).
Targets&IC50 CTX-M-15:5 nM , TEM-1:8 nM
In vitro Avibactam inhibits class A and C β-lactamases. Avibactam inactivates the most important β-lactamases except metallo types and Acinetobacter OXA carbapenemases [2].
In vivo Avibactam sodium displays a slow return of activity with an off-rate of 0.045±0.022/min, 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]. 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 liters/kg (SD, 0.14 liters/kg) and 1.18 liters/kg (SD, 0.34 liters/kg), respectively [3].
Synonyms NXL-104 free acid
Molecular Weight 265.24
Formula C7H11N3O6S
CAS No. 1192500-31-4

Storage

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

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.

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Keywords

Avibactam free acid 1192500-31-4 Microbiology/Virology Antibacterial NXL-104 free acid inhibitor inhibit

 

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