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Avibactam sodium β-lactamase inhibitor

Cat.No.S3732

Avibactam (AVE-1330A, NXL104) is a covalent, reversible, non-β-lactam β-lactamase inhibitor with IC50 values of 8, 80, and 38 nM for TEM-1, P99, and KPC-2 β-lactamases, respectively.
Avibactam sodium β-lactamase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 287.23

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 287.23 Formula

C7H10N3O6 .Na

Storage (From the date of receipt)
CAS No. 1192491-61-4 Download SDF Storage of Stock Solutions

Synonyms AVE-1330A, NXL104 Smiles C1CC(N2CC1N(C2=O)OS(=O)(=O)[O-])C(=O)N.[Na+]

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (198.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 57 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
SHV-4 [1]
(Cell-free assay)
1.5 nM
TEM-1 [1]
(Cell-free assay)
8 nM
KPC-2 [1]
(Cell-free assay)
38 nM
P99 [1]
(Cell-free assay)
80 nM
In vitro
Avibactam (formerly NXL104, AVE1330A) is a synthetic non-β-lactam, β-lactamase inhibitor inhibits the activities of Ambler class A and C β-lactamases and some Ambler class D enzymes[1]. Avibactam has an unusual mechanism of action: it is a covalent inhibitor that acts via ring opening, but in contrast to other currently used β-lactamase inhibitors, this reaction is reversible[2].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01448395 Completed
Healthy
Pfizer
October 2011 Phase 1
NCT01291602 Completed
Healthy Male and Female Japanese Volunteers
Pfizer
February 2011 Phase 1

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