2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial Topoisomerase Antibiotic
  4. Trovafloxacin mesylate

Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.

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Trovafloxacin mesylate Chemical Structure

Trovafloxacin mesylate Chemical Structure

CAS No. : 147059-75-4

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Based on 2 publication(s) in Google Scholar

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Trovafloxacin mesylate Related Antibodies

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam

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Description

Trovafloxacin mesylate is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin mesylate is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1[1][2][3].

IC50 & Target

Quinolone

 

In Vitro

Trovafloxacin (20 µM; 24 hours; HepG2 cells) and tumor necrosis factor (TNF; 4 ng/mL) incubation induces apoptosis and increases leakage of lactate dehydrogenase (LDH) in HepG2 cells[1].
Trovafloxacin (20 µM; 24 hours; HepG2 cells) and TNF (4 ng/mL) incubation increases expression of early NF-κB-related factors A20 and IκBα[1].
Trovafloxacin prolongs TNF-induced activation of MAPKs and IKKα/β activation in HepG2[1].
Trovafloxacin is a potent inhibitor of TO-PRO-3 uptake by apoptotic cells. Trovafloxacin also inhibits ATP release from apoptotic cells. Trovafloxacin does not inhibit caspase 3/7 activation, or caspase-mediated PANX1 cleavage during apoptosis[2].
Trovafloxacin is equally active against both penicillin-susceptible and -resistant pneumococci, with MICs of 0.06-0.25 mg/mL reported for more than 700 isolates. The MICs of Trovafloxacin at which 90% of isolates are inhibited for 55 isolates of pneumococci is 0.125 μg/mL[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Trovafloxacin mesylate Related Antibodies

Apoptosis Analysis[1]

Cell Line: HepG2 cells
Concentration: 20 µM
Incubation Time: 24 hours
Result: Showed a gradual increase of Annexin V-staining and an increased leakage of lactate dehydrogenase (LDH) at 24 h.

RT-PCR[1]

Cell Line: HepG2 cells
Concentration: 20 µM
Incubation Time: 24 hours
Result: Caused a higher increase in the transcription of A20 and IκBα in HepG2 cells.
In Vivo

Trovafloxacin (150 mg/kg; oral administration; male C57BL/6 J mice) treatment disrupts TNF-induced p65 nuclear translocation. Trovafloxacin treatment increases expression of early NF-κB-related factors A20 and IκBα[1].
Trovafloxacin, when administered in combination with lipopolysaccharide (LPS) or TNF to mice induces severe liver toxicity associated with vast apoptotic areas in the liver, increased serum levels of alanine amino transferases (ALT) and pro-inflammatory cytokines[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 J mice (9-11-week-old) injected with recombinant murine TNF ion[1]
Dosage: 150 mg/kg
Administration: Oral administration; once
Result: Showed a greater number of cells with increased nuclear/cytoplasmic p65 ratio in liver.
Clinical Trial
Molecular Weight

512.46

Formula

C21H19F3N4O6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CN(C2=CC=C(F)C=C2F)C3=NC(N4C[C@@]5([H])[C@H](N)[C@@]5([H])C4)=C(F)C=C3C1=O)O.CS(=O)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (243.92 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (39.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9514 mL 9.7569 mL 19.5137 mL
5 mM 0.3903 mL 1.9514 mL 3.9027 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.06 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.56%

COA (254 KB) HNMR (307 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.9514 mL 9.7569 mL 19.5137 mL 48.7843 mL
5 mM 0.3903 mL 1.9514 mL 3.9027 mL 9.7569 mL
10 mM 0.1951 mL 0.9757 mL 1.9514 mL 4.8784 mL
15 mM 0.1301 mL 0.6505 mL 1.3009 mL 3.2523 mL
20 mM 0.0976 mL 0.4878 mL 0.9757 mL 2.4392 mL
25 mM 0.0781 mL 0.3903 mL 0.7805 mL 1.9514 mL
30 mM 0.0650 mL 0.3252 mL 0.6505 mL 1.6261 mL
DMSO 40 mM 0.0488 mL 0.2439 mL 0.4878 mL 1.2196 mL
50 mM 0.0390 mL 0.1951 mL 0.3903 mL 0.9757 mL
60 mM 0.0325 mL 0.1626 mL 0.3252 mL 0.8131 mL
80 mM 0.0244 mL 0.1220 mL 0.2439 mL 0.6098 mL
100 mM 0.0195 mL 0.0976 mL 0.1951 mL 0.4878 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trovafloxacin147059-75-4BacterialTopoisomeraseAntibioticPANX1antibioticbroad-spectrumhepatotoxicityNF-κBLPSpro-inflammatoryTNFDNAgyrasetopoisomerase-IVpneumococciInhibitorinhibitorinhibit

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