Avibactam (sodium salt) (Synonyms: AVE-1330A, NXL104) |
Catalog No.GC42883
One-Click Copy Product Info
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Avibactam (sodium salt) (NXL104, AVE1330A) is a covalent, reversible inhibitor of non-β-lactam β-lactamases. It effectively inhibits β-lactamase TEM-1 and CTX-M-15 with IC50 values of 8 nM and 5 nM, respectively. Avibactam is active against Ambler class A and C β-lactamases and also shows activity against certain Ambler class D enzymes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1192491-61-4
Sample solution is provided at 25 µL, 10mM.
Avibactam (sodium salt) (NXL104, AVE1330A) is a covalent, reversible inhibitor of non-β-lactam β-lactamases. It effectively inhibits β-lactamase TEM-1 and CTX-M-15 with IC50 values of 8 nM and 5 nM, respectively. Avibactam is active against Ambler class A and C β-lactamases and also shows activity against certain Ambler class D enzymes. The mechanism of action of Avibactam is the formation of stable, irreversible covalent bonds at the active site of class A or class C beta-lactamases, resulting in permanent inactivation of the enzyme[1-3].
Avibactam (sodium salt) at a fixed concentration of 4 μg/ml dramatically improves the activities of cephalosporins against Enterobacteriaceae resistant to these agents by means of ESBL and AmpC β-lactamases[4-5].
Avibactam (sodium salt) and ceftazidime had bactericidal effects in infected with ceftazidime resistant Pseudomonas aeruginosa mice[6]. The addition of the beta-lactamase inhibitor avibactam (2-256 mg/kg; s.c; twice a day for five days) to ceftazidime restored the efficacy of ceftazidime in a mouse model of acute fatal septicemia in mice[7].
References:
[1]. Ehmann DE, Jahić H, 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. doi: 10.1073/pnas.1205073109. Epub 2012 Jul 2. PMID: 22753474; PMCID: PMC3406822.
[2]. Bhattacharya S, Bonnet A, et,al. inventors; Novexel SA and Forest laboratories holdings, assignees. Polymorphic and pseudopolymorphic forms of a pharmaceutical compound. International patent WO 042560 A2. 2011 April 14.
[3]. Stachyra T, Péchereau MC, et,al. Mechanistic studies of the inactivation of TEM-1 and P99 by NXL104, a novel non-beta-lactam beta-lactamase inhibitor. Antimicrob Agents Chemother. 2010 Dec;54(12):5132-8. doi: 10.1128/AAC.00568-10. Epub 2010 Oct 4. PMID: 20921316; PMCID: PMC2981269.
[4]. Lagacé-Wiens PR, Tailor F, et,al. Activity of NXL104 in combination with beta-lactams against genetically characterized Escherichia coli and Klebsiella pneumoniae isolates producing class A extended-spectrum beta-lactamases and class C beta-lactamases. Antimicrob Agents Chemother. 2011 May;55(5):2434-7. doi: 10.1128/AAC.01722-10. Epub 2011 Feb 28. PMID: 21357295; PMCID: PMC3088241.
[5]. Sader HS, Castanheira M, et,al. Antimicrobial activity of ceftazidime-avibactam against Gram-negative organisms collected from U.S. medical centers in 2012. Antimicrob Agents Chemother. 2014;58(3):1684-92. doi: 10.1128/AAC.02429-13. Epub 2013 Dec 30. PMID: 24379201; PMCID: PMC3957905.
[6]. Berkhout J, Melchers MJ, et,al. Pharmacokinetics and penetration of ceftazidime and avibactam into epithelial lining fluid in thigh- and lung-infected mice. Antimicrob Agents Chemother. 2015 Apr;59(4):2299-304. doi: 10.1128/AAC.04627-14. Epub 2015 Feb 2. PMID: 25645843; PMCID: PMC4356781.
[7]. Endimiani A, Hujer KM, et,al. Evaluation of ceftazidime and NXL104 in two murine models of infection due to KPC-producing Klebsiella pneumoniae. Antimicrob Agents Chemother. 2011 Jan;55(1):82-5. doi: 10.1128/AAC.01198-10. Epub 2010 Nov 1. PMID: 21041503; PMCID: PMC3019638.
| Cell experiment [1]: | |
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Cell lines |
K. pneumonia (ESBL-producing) |
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Preparation Method |
The bactericidal activity of cefepime in vitro with or without avibactam at 4 μg/ml was determined by broth microdilution method. |
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Reaction Conditions |
4 μg/ml |
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Applications |
Avibactam significantly increased the activity of cefepime against ESBL-producing strains, restoring 100% susceptibility to ESBL-producing organism. |
| Animal experiment [2]: | |
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Animal models |
CD-1 mice |
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Preparation Method |
Mice were infected by the intraperitoneal injection of the KPC-producing K. pneumoniae strain resulting in the death of untreated controls within 24 to 48 h.Thirty minutes postinfection, a single subcutaneous dose of ceftazidime with and without avibactam was initiated, and the survival ratio was monitored for 5 days twice a day. |
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Dosage form |
2-256 mg/kg; s.c; twice a day for five days |
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Applications |
The addition of avibactam significantly reduced the amount of ceftazidime (CAZ) required to treat systemic infections in mice. |
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References: |
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| Cas No. | 1192491-61-4 | SDF | |
| Synonyms | AVE-1330A, NXL104 | ||
| Chemical Name | sulfuric acid, mono[(1R,2S,5R)-2-(aminocarbonyl)-7-oxo-1,6-diazabicyclo[3.2.1]oct-6-yl] ester, monosodium salt | ||
| Canonical SMILES | NC([C@H]1[N@@](C2)C(N(OS([O-])(=O)=O)[C@@H]2CC1)=O)=O.[Na+] | ||
| Formula | C7H10N3O6S•Na | M.Wt | 287.2 |
| Solubility | 5mg/mL in DMSO, or in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4819 mL | 17.4095 mL | 34.8189 mL |
| 5 mM | 696.4 μL | 3.4819 mL | 6.9638 mL |
| 10 mM | 348.2 μL | 1.7409 mL | 3.4819 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)