This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
Metallo-β-lactamase-IN-6
Catalog No. T60239 CAS
1439899-44-1
Metallo-β-lactamase-IN-6 is a highly effective inhibitor of VIM-Type metallo-β-lactamase, demonstrating IC 50 values of 0.56 μM, 29.50 μM, and 5.78 μM for VIM-2, VIM-1, and VIM-5, respectively. In addition, Metallo-β-lactamase-IN-6 exhibits potent synergistic antibacterial properties when combined with Meropenem, particularly against engineered Escherichia coli strains and clinically isolated Pseudomonas aeruginosa carrying the VIM-2 MBL gene [1].
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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.
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Biological Description
Chemical Properties
Storage
& Solubility Information
Description
Metallo-β-lactamase-IN-6 is a highly effective inhibitor of VIM-Type metallo-β-lactamase, demonstrating IC 50 values of 0.56 μM, 29.50 μM, and 5.78 μM for VIM-2, VIM-1, and VIM-5, respectively. In addition, Metallo-β-lactamase-IN-6 exhibits potent synergistic antibacterial properties when combined with Meropenem, particularly against engineered Escherichia coli strains and clinically isolated Pseudomonas aeruginosa carrying the VIM-2 MBL gene [1].
In vitro
Metallo-β-lactamase-IN-6 (compound 55) (10 μM; 18-20 hours) enhances Meropenem's efficacy against VIM-2 mediated antibacterial resistance, evidenced by FIC index values of 0.05 [1]. At concentrations of 1, 10, and 100 μM over 18-20 hours, it can breach the E. coli outer membrane, consequently revitalizing Meropenem's action against PBP3 by neutralizing the VIM-2 enzyme's adverse impact on Meropenem [1]. Furthermore, at 100 μM, it boosts Meropenem's antibacterial potency against PA W35, as indicated by FIC index values of 0.25 [1].
In vivo
Administered intraperitoneally at a single dose of 100 mg/kg, Metallo-β-lactamase-IN-6 reaches a peak plasma concentration of approximately 142.8 μg/mL around 9 minutes post-injection, with a half-life of 1.24 hours, indicating swift systemic availability and moderate persistence in the body [1]. When administered as a single intraperitoneal dose of 500, 1000, or 2000 mg/kg, Metallo-β-lactamase-IN-6 displayed no significant toxic effects and was well-tolerated in female ICR mice up to the highest tested dose of 2000 mg/kg over a 14-day observation period. These findings suggest that Metallo-β-lactamase-IN-6 is quickly absorbed and metabolized, with a favorable safety profile in the tested mouse model [1].
Molecular Weight
203.2
Formula
C10H9N3O2
CAS No.
1439899-44-1
Storage
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dose Conversion
You can also refer to dose conversion for different animals.
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Method for preparing DMSO master liquid: mg
drug pre-dissolved in μL DMSO (Master liquid concentration
mg/mL),
Method for preparing in vivo formulation:Take μL
DMSO master liquid, next add μL PEG300, mix and clarify, next add μL
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:
Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.