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Avibactam sodium

Cat. No. M6174
Avibactam sodium Structure
Synonym:

NXL-104

Size Price Availability Quantity
10mg USD 300 In stock
50mg USD 880 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: Avibactam (NXL104) sodium is a molecule with little antibacterial activity, that inhibits class A and C β-lactamases. Avibactam inactivates most important β-lactamases except metallo types and Acinetobacter OXA carbapenemases.

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. 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]. Avibactam is a new promising β-lactamase inhibitor, to overcome resistance caused by β-lactamases. 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 287.23
Formula C7H10N3NaO6S
CAS Number 1192491-61-4
Purity >99%
Solubility 30 mg/mL in DMSO
Storage at -20°C
References

β-Lactamase inhibition by avibactam in Mycobacterium abscessus.
Dubée V, et al. J Antimicrob Chemother. 2015 Apr;70(4):1051-8. PMID: 25525201.

Unexpected in vivo activity of ceftazidime alone and in combination with avibactam against New Delhi metallo-β-lactamase-producing Enterobacteriaceae in a murine thigh infection model.
MacVane SH, et al. Antimicrob Agents Chemother. 2014 Nov;58(11):7007-9. PMID: 25223998.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Avibactam sodium, NXL-104 supplier, inhibitors

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