Trovafloxacin
Based on 8 publication(s) in Google Scholar
Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive, Gram-negative and anaerobic organisms. Trovafloxacin blocks the DNA gyrase and topoisomerase IV activity. Trovafloxacin is also a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. Trovafloxacin does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin leads to dysregulated fragmentation of apoptotic cells by inhibiting PANX1.
For research use only. We do not sell to patients.
- Purity : 99.43%
- CAS No.: 147059-72-1
- Formula: C20H15F3N4O3
- Molecular Weight:416.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Trovafloxacin
More- Nat Neurosci. 2024 Aug;27(8):1522-1533. [Abstract]
- Acta Pharm Sin B. 2025 Dec;15(12):6382-6398. [Abstract]
- Ecotoxicol Environ Saf. 2025 Nov 15:307:119433. [Abstract]
- Clin Transl Sci. 2025 Nov;18(11):e70400. [Abstract]
- Biotechnol Bioeng. 2021 Dec;118(12):4687-4698. [Abstract]
- J Gen Physiol. 2025 Jan 6;157(1):e202413676. [Abstract]
- bioRxiv. 2026 Jul 17:2026.07.12.738047.
- bioRxiv. 2024 Nov 06.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
All Topoisomerase Isoforms
MoreAll Antibiotic Isoforms
More
Biological Activity
Description
IC50 & Target
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Quinolone |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
11.16 μg/mL
Compound: Trovafloxacin
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Cytotoxicity was determined for the compound in HepG2 cell line
Cytotoxicity was determined for the compound in HepG2 cell line
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[PMID: 14980680] |
| MC3T3-E1 | IC50 |
<1.2 μM
Compound: Trovafloxacin
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Inhibition of mouse MC3T3-E1 cell proliferation after 48 to 72 hrs
Inhibition of mouse MC3T3-E1 cell proliferation after 48 to 72 hrs
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[PMID: 19595598] |
| MRC5 | IC50 |
0.96 μM
Compound: TVFX (trovafloxacin)
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In vitro inhibitory activity on MRC5 fibroblast tissue cultures inoculated with virulent RH strain of Toxoplasma gondii
In vitro inhibitory activity on MRC5 fibroblast tissue cultures inoculated with virulent RH strain of Toxoplasma gondii
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[PMID: 15125930] |
| NIH3T3 | IC50 |
244.28 μg/mL
Compound: Trovafloxacin
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Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell proliferation after 24 hrs by MTT assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell proliferation after 24 hrs by MTT assay
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[PMID: 28174104] |
| V79-4 | IC50 |
3.77 μg/mL
Compound: Trovafloxacin
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Cytotoxicity was determined for the compound in V79-4 cell line
Cytotoxicity was determined for the compound in V79-4 cell line
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[PMID: 14980680] |
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.
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Cell Line:HepG2 cells
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Concentration:20 µM
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Incubation Time:24 hours
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Result:Showed a gradual increase of Annexin V-staining and an increased leakage of lactate dehydrogenase (LDH) at 24 h.
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Cell Line:HepG2 cells
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Concentration:20 µM
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Incubation Time:24 hours
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Result:Caused a higher increase in the transcription of A20 and IκBα in HepG2 cells.
In Vivo
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.
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Animal Model:Male C57BL/6 J mice (9-11-week-old) injected with recombinant murine TNF ion[1]
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Dosage:150 mg/kg
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Administration:Oral administration
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Result:Showed a greater number of cells with increased nuclear/cytoplasmic p65 ratio in liver.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 147059-72-1
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Appearance Solid
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Molecular Weight 416.35
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Formula C20H15F3N4O3
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Color White to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
Spatiotemporally selective astrocytic ATP dynamics encode injury information sensed by microglia following brain injury in mice. [Abstract]2024 Aug;27(8):1522-1533. PMID: 38862791 -
Acta Pharm Sin B
2025 Dec;15(12):6382-6398. PMID: 41477334
Trovafloxacin purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2025 Dec;15(12):6382-6398. [Abstract]
Trovafloxacin (0-100 μM) showed cytotoxicity in SB-HEO, SB-HEO-DM, HepG2 cells, PHHs, and 2D HLCs in a dose-dependent manner.
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Ecotoxicol Environ Saf
PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]2025 Nov 15:307:119433. PMID: 41273832
Trovafloxacin purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2025 Nov 15:307:119433. [Abstract]
Trovafloxacin (10, 20, 40, 80, 100 μM; 24 h) inhibited cell viability of A549 cells.
Trovafloxacin purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2025 Nov 15:307:119433. [Abstract]
Trovafloxacin (10, 20, 40, 80, 100 μM; 24 h)showed no significant differences in relative luciferase activity when compared with the control in A549 cells.
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Clin Transl Sci
Evaluation of Elexacaftor/Tezacaftor/Ivacaftor-Mediated Drug-Induced Liver Injury Using a Liver-On-Chip Model. [Abstract]2025 Nov;18(11):e70400. PMID: 41222452 -
Biotechnol Bioeng
An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]2021 Dec;118(12):4687-4698. PMID: 34478150 -
J Gen Physiol
Distinct properties and activation of hexameric and heptameric Pannexin 1 channel concatemers. [Abstract]2025 Jan 6;157(1):e202413676. PMID: 39704698 -
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Solvent & Solubility
In Vitro:
DMSO : 10 mg/mL (24.02 mM; ultrasonic and adjust pH to 2 with 1M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1 mg/mL (2.40 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1 mg/mL (2.40 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Giustarini G, et al. The hepatotoxic fluoroquinolone trovafloxacin disturbs TNF- and LPS-induced p65 nuclear translocation in vivo and in vitro. Toxicol Appl Pharmacol. 2020 Mar 15;391:114915. [Content Brief]
[2]. Poon IK, et al. Unexpected link between an antibiotic, pannexin channels and apoptosis. Nature. 2014 Mar 20;507(7492):329-34. [Content Brief]
[3]. Gootz TD, et al. Activity of the new fluoroquinolone trovafloxacin (CP-99,219) against DNA gyrase and topoisomerase IV mutants of Streptococcus pneumoniae selected in vitro. Antimicrob Agents Chemother. 1996 Dec;40(12):2691-7. [Content Brief]
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4018 mL | 12.0091 mL | 24.0183 mL | 60.0456 mL |
| 5 mM | 0.4804 mL | 2.4018 mL | 4.8037 mL | 12.0091 mL | |
| 10 mM | 0.2402 mL | 1.2009 mL | 2.4018 mL | 6.0046 mL | |
| 15 mM | 0.1601 mL | 0.8006 mL | 1.6012 mL | 4.0030 mL | |
| 20 mM | 0.1201 mL | 0.6005 mL | 1.2009 mL | 3.0023 mL |
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