Avibactam sodium

Research use only, not for human use.

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

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

Avibactam is a molecule with little antibacterial activity, that inhibits class A and C β-lactamases, but not metallo types and Acinetobacter OXA carbapenemases. 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.

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.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. Animal Model:Six-week-old BALB/c mice (female), K. pneumoniae strain Y8 infection model Dosage:0.375?mg/g in combination with Ceftazidime Administration:Subcutaneous injection, 4?h post infection and given every 8?h for 10?days Result:70% of infection group mice died within 4?days, and all mice in the PBS group died within 13?days. All treatment group mice survived at 10 days post infection with the antibiotic applied every 8?h, whereas 100% of mice in this group died within 4?days after the antibiotic treatment stopped. The spleen and liver of treatment group mice showed lower CFU counts, as compare with that of infected group.

NXL-104

Others

Other Targets

CTX-M-15| KPC-2 β-lactamases| P99 β-lactamases| TEM-1 β-lactamases

Infection

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1192491-61-4

287.22

C7H10N3NaO6S

>98% (HPLC)

H2O : ≥ 145 mg/mL 504.82 mM; DMSO : ≥ 30 mg/mL 104.45 mM

C1C[C@H](N2C[C@@H]1N(C2=O)OS(=O)(=O)[O-])C(=O)N.[Na+]

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(-20℃)

With Ice Pack

≥ 2 years