2. Trovafloxacin

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.

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Trovafloxacin Chemical Structure

Trovafloxacin Chemical Structure

CAS No. : 147059-72-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Trovafloxacin:

Trovafloxacin Related Antibodies

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Description

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[1][2][3].

IC50 & Target

IC50: 4 μM (Pannexin 1 channel (PANX1))[2]
Gram-positive, Gram-negative and anaerobic organisms[3]
DNA gyrase[3]
Topoisomerase IV[3]
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 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
Result: Showed a greater number of cells with increased nuclear/cytoplasmic p65 ratio in liver.
Clinical Trial
Molecular Weight

416.35

Formula

C20H15F3N4O3
CAS No.
Appearance

Solid

Color

White to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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)

DMSO : 9.09 mg/mL (21.83 mM; ultrasonic and adjust pH to 3 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4018 mL 12.0091 mL 24.0183 mL
5 mM 0.4804 mL 2.4018 mL 4.8037 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

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 / 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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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:

Trovafloxacin147059-72-1Inhibitorinhibitorinhibit

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