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Purity: ≥98%
Avibactam (NXL-104; NXL104; Avycaz) is a covalent/reversible non-β-lactam β-lactamase inhibitor approved for use in combination with ceftazidime by the FDA on February 25, 2015 for treating bacterial infections, including those caused by multi-drug resistant gram-negative bacterial pathogens. It inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively.
| Targets |
CTX-M-15(IC50=5 nM);TEM-1(IC50=8 nM )
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| ln Vitro |
Monetary antibacterial activity is low for avibactam, which inhibits class A and C β-lactamases but not metallotypes or Acinetobacter OXA carbapenemases[2].
With MIC50 and MIC90 for both 8 mg/L, ceftazidime (HY-B0593)-avibactam (0-256 mg/L) inhibits the growth of 16 blaKPC-2 positive and 1 blaOXA-232 positive Klebsiella pneumonia[4]. |
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| ln Vivo |
Ceftazidime-Avibactam (0.375 mg/g; s.c.; every 8 hours for 10 days) significantly affects the bacteria and has been shown to have some therapeutic efficacy in an infected mouse model with K. pneumoniae strain Y8[3].
Avibactam (64 mg/kg; s.c.; once) infected neutropenic mice with lung infection exhibits a mean estimated half-life in plasma in the terminal phase of 0.24 h[3].
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| Animal Protocol |
Animal Model: Six-week-old BALB/c mice (female), K. pneumoniae strain Y8 infection model[4]
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: Within 4 days, 70% of the mice in the infection group perished, and in 13 days, every mouse in the PBS group perished. When the antibiotic was given every eight hours for ten days after infection, all of the mice in the treatment group survived; however, when the antibiotic treatment was stopped, all of the mice in the control group perished in four days. When compared to the infected group, the treatment group mice's liver and spleen had reduced CFU counts. |
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| References |
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| Molecular Formula |
C7H10N3NAO6S
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| Molecular Weight |
287.22
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| Elemental Analysis |
C, 29.27; H, 3.51; N, 14.63; Na, 8.00; O, 33.42; S, 11.16
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| CAS # |
1192491-61-4
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| Related CAS # |
Avibactam free acid;1192500-31-4;Avibactam sodium hydrate;2938989-90-1;Avibactam sodium dihydrate
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| Appearance |
Solid powder
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| SMILES |
O=C1N(OS(=O)(O[Na])=O)[C@H]2CN1[C@H](C(N)=O)CC2
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| InChi Key |
RTCIKUMODPANKX-JBUOLDKXSA-M
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| InChi Code |
InChI=1S/C7H11N3O6S.Na/c8-6(11)5-2-1-4-3-9(5)7(12)10(4)16-17(13,14)15;/h4-5H,1-3H2,(H2,8,11)(H,13,14,15);/q;+1/p-1/t4-,5+;/m1./s1
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| Chemical Name |
sodium (2S,5R)-2-carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl sulfate
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| Synonyms |
NXL104; NXL-104; NXL 104; Avibactam;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :30~57 mg/mL ( 104.45 ~198.44 mM )
Water : 50 ~57 mg/mL(~174.08 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (9.57 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (9.57 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (7.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 5: ≥ 0.55 mg/mL (1.91 mM) (saturation unknown) in 1% DMSO 99% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 6: 5% DMSO+40% PEG300+5% Tween-80+50% Saline: ≥ 2.75 mg/mL (9.57 mM) Solubility in Formulation 7: 140 mg/mL (487.41 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4817 mL | 17.4083 mL | 34.8165 mL | |
| 5 mM | 0.6963 mL | 3.4817 mL | 6.9633 mL | |
| 10 mM | 0.3482 mL | 1.7408 mL | 3.4817 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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