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.
TP0480066
Catalog No. T61481 CAS
2245693-15-4
TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topo IV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2].
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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
TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topo IV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2].
In vitro
TP0480066 (compound 32) has demonstrated notable antimicrobial efficacy within concentrations of 0-2048 μg/mL over 18-24 hours, showcasing robust activity against a variety of bacterial species, including drug-resistant strains like MRSA (n=24), gPRSP (n=30), and VRE (n=34), as well as against Clostridioides difficile. Moreover, within a 24-48 hour timeframe, TP0480066 has shown potent activity against N. gonorrhoeae, including those strains exhibiting decreased susceptibility or resistance to existing antimicrobial agents. Specifically, at concentrations of 1.25×10^-4, 5×10^-4, and 2×10^-3 μg/mL over 24 hours, it displayed effective time-kill activity against N. gonorrhoeae ATCC 49226, significantly reducing its viable counts. Cell viability assays further confirmed TP0480066's broad-spectrum antimicrobial potential, illustrating favorable activities against clinically isolated methicillin-resistant S. aureus, vancomycin-resistant enterococci (including E. faecium and E. faecalis), and genotype penicillin-resistant S. pneumonia with minimum inhibitory concentration (MIC) ranges indicative of high efficacy. Additionally, against various N. gonorrhoeae strains, including ATCC and NCTC lines, TP0480066 exhibited significant antimicrobial activities at exceptionally low MIC values, highlighting its potential as a formidable agent against both standard and drug-resistant bacterial pathogens.
In vivo
Administered subcutaneously at a dose of 100 mg/kg, TP0480066 demonstrates significant pharmacokinetic parameters in female Slc:ICR mice, achieving a peak concentration (C max) of 12400 ng/mL at 0.250 hours (T max), with a half-life (t 1/2) of 6.79 hours, and an area under the concentration-time curve (AUC) from 0 to 24 hours of 16000 ng×h/mL. Additionally, in a dose-dependent manner, TP0480066, at dosages of 1, 3, 10, 30, and 100 mg/kg, markedly inhibits the growth of N. gonorrhoeae ATCC 49226 and NCTC 13479 in female BALB/c mice with genital tract infections, showing significant effectiveness at 30 and 100 mg/kg doses. These outcomes are drawn from studies employing subcutaneous injections in single doses across different concentrations, highlighting TP0480066's potential against N. gonorrhoeae infections.
Molecular Weight
371.32
Formula
C18H14FN3O5
CAS No.
2245693-15-4
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.