Vaborbactam (Synonyms: RPX 7009) |
Catalog No.GC19369
One-Click Copy Product Info
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Vaborbactam (RPX7009) is a broad-spectrum β-lactamase inhibitor with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1360457-46-0
Sample solution is provided at 25 µL, 10mM.
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Vaborbactam (RPX7009) is a broad-spectrum β-lactamase inhibitor with particularly potent activity against KPC, CTX-M, SHV, and CMY enzymes[1]. Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase competitive inhibitor used to treat complicated urinary tract infections[2]. Vaborbactam forms a reversible coordination bond with β-lactamases and is not hydrolyzed by β-lactamases[3]. Vaborbactam can enhance the activity of β-lactams against Mycobacterium abscessus[4]. Vaborbactam is often used in combination with Meropenem and has potent in vitro activity against resistant Gram-negative pathogens, especially Klebsiella pneumoniae that produces Klebsiella pneumoniae carbapenemase (KPC), with MIC50 values typically ≤ 0.06µg/ml[5].
In vivo, vaborbactam (6.25-100mg/kg) was injected intraperitoneally in mice to treat a 24-hour thigh infection model of Klebsiella pneumoniae KP1094. Combining it with two meropenem regimens (100 and 300mg/kg) produced a dose-dependent bactericidal effect, with a maximum bactericidal effect of 2.50 log CFU/thigh[6].
References:
[1] Hamrick J C, Docquier J D, Uehara T, et al. VNRX-5133 (taniborbactam), a broad-spectrum inhibitor of serine-and metallo-β-lactamases, restores activity of cefepime in Enterobacterales and Pseudomonas aeruginosa[J]. Antimicrobial Agents and Chemotherapy, 2020, 64(3): 10.1128/aac. 01963-19.
[2] Iqbal Z, Sun J, Yang H, et al. Recent developments to cope the antibacterial resistance via β-lactamase inhibition[J]. Molecules, 2022, 27(12): 3832.
[3] Bookser B C, Reddy K R, Boyer S H, et al. Vaborbactam (in Combination with Meropenem as Vabomere), a Non‐β‐Lactam β‐Lactamase Inhibitor for Treatment of Complicated Urinary Tract Infections and Pyelonephritis[J]. Current Drug Synthesis, 2022: 17-40.
[4] Sanchez L, Bitar M, Herail Q, et al. In vitro and intracellular activity of vaborbactam combined with β-lactams against Mycobacterium abscessus[J]. Journal of Antimicrobial Chemotherapy, 2024, 79(8): 1914-1918.
[5] Wenzler E, Scoble P J. An appraisal of the pharmacokinetic and pharmacodynamic properties of meropenem-vaborbactam[J]. Infectious Diseases and Therapy, 2020, 9(4): 769-784.
[6] Sabet M, Tarazi Z, Nolan T, et al. Activity of meropenem-vaborbactam in mouse models of infection due to KPC-producing carbapenem-resistant Enterobacteriaceae[J]. Antimicrobial Agents and Chemotherapy, 2018, 62(1): 10.1128/aac. 01446-17.
| Animal experiment [1]: | |
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Animal models |
Female Swiss Webster mice |
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Preparation Method |
A 24-hour thigh infection model was established using Klebsiella pneumoniae KP1094. After infection, mice were treated with 100 or 300 mg/kg meropenem intraperitoneally every 2 hours for 24 hours alone or in combination with Vaborbactam ranging from 6.25 to 100 mg/kg every 2 hours for 24 hours. |
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Dosage form |
6.25 to 100mg/kg; i.p. |
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Applications |
The addition of Vaborbactam to both meropenem regimens produced bacterial killing in a dose-dependent fashion, with a maximum of bacterial killing of 2.50 log CFU/thigh. |
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References: [1]Sabet M, Tarazi Z, Nolan T, et al. Activity of meropenem-vaborbactam in mouse models of infection due to KPC-producing carbapenem-resistant Enterobacteriaceae[J]. Antimicrobial Agents and Chemotherapy, 2018, 62(1): 10.1128/aac. 01446-17. |
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| Cas No. | 1360457-46-0 | SDF | |
| Synonyms | RPX 7009 | ||
| Canonical SMILES | O=C(O)C[C@@H]1CC[C@H](NC(CC2=CC=CS2)=O)B(O)O1 | ||
| Formula | C12H16BNO5S | M.Wt | 297.14 |
| Solubility | Water : 5.26 mg/mL (17.70 mM) | 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 | 3.3654 mL | 16.8271 mL | 33.6542 mL |
| 5 mM | 673.1 μL | 3.3654 mL | 6.7308 mL |
| 10 mM | 336.5 μL | 1.6827 mL | 3.3654 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 23 reference(s) in Google Scholar.)