For research use only. Not for therapeutic Use.
Avibactam sodium (NXL-104) hydrate 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[1].
Avibactam is a molecule with little antibacterial activity, that inhibits class A and C β-lactamases, but not metallo types and Acinetobacter OXA carbapenemases[2].
Ceftazidime (HY-B0593)-Avibactam (0-256 mg/L) inhibits 16 blaKPC-2 positive and 1 of blaOXA-232 positive Klebsiella pneumonia growth with MIC50 and MIC90 for both 8 mg/L[4].
Ceftazidime-Avibactam (0.375 mg/g; s.c.; q8h for 10 days) has a significant effect on the bacteria and led to a certain therapeutic efficacy in K. pneumoniae strain Y8 infected mouse model[3].
Avibactam (64 mg/kg; s.c.; once) shows mean estimated half-life in plasma in the terminal phase of 0.24 h in Pseudomonas aeruginosa infected neutropenic mice with lung infection[3].
| Catalog Number | I046379 |
| CAS Number | 2938989-90-1 |
| Synonyms | sodium;[(2S,5R)-2-carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] sulfate;hydrate |
| Molecular Formula | C7H12N3NaO7S |
| Purity | ≥95% |
| InChI | InChI=1S/C7H11N3O6S.Na.H2O/c8-6(11)5-2-1-4-3-9(5)7(12)10(4)16-17(13,14)15;;/h4-5H,1-3H2,(H2,8,11)(H,13,14,15);;1H2/q;+1;/p-1/t4-,5+;;/m1../s1 |
| InChIKey | QTECZIOYYRSGNA-CIFXRNLBSA-M |
| SMILES | C1CC(N2CC1N(C2=O)OS(=O)(=O)[O-])C(=O)N.O.[Na+] |
| Reference | [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 GR20263 and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrob Agents Chemother. 2015 Apr;59(4):2299-304. [4]. Zhang W, et al. In vitro and in vivo bactericidal activity of ceftazidime-avibactam against Carbapenemase-producing Klebsiella pneumoniae. Antimicrob Resist Infect Control. 2018 Nov 21;7:142. |
