Avibactam sodium hydrate | HY-14879B

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].

IC₅₀ & Target:

IC50: 5 nM (CTX-M-15), 8 nM (TEM-1)[1]

In Vitro:

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 bla_KPC-2 positive and 1 of bla_OXA-232 positive Klebsiella pneumonia growth with MIC₅₀ and MIC₉₀ for both 8 mg/L^[4].

In Vivo:

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].

Formule:

C7H12N3NaO7S

SMILES:

O=S(ON1[C@]2([H])CC[C@@H](C(N)=O)[N@@](C2)C1=O)(O[Na])=O.O

Stockage:

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)