Trovafloxacin

SKU: orb1219815

Description

Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive. In HepG2 cells, Trovafloxacin (20 μM; 24 hours; ) and tumor necrosis factor (TNF; 4 ng/mL) incubation induces apoptosis and increases leakage of lactate dehydrogenase (LDH). Trovafloxacin (20 μM; 24 hours; HepG2 cells) and TNF (4 ng/mL) incubation increases expression of early NF-κB-related factors A20 and IκBα. Trovafloxacin prolongs TNF-induced activation of MAPKs and IKKα/β activation in HepG2. Trovafloxacin is a potent TO-PRO-3 uptake inhibitor by apoptotic cells. Trovafloxacin also inhibits ATP release from apoptotic cells. 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.In male C57BL/6 J mice, TNF-induced p65 nuclear translocation disrupted by Trovafloxacin (150 mg/kg; oral administration). Trovafloxacin treatment increases expression of early NF-κB-related factors A20 and IκBα. Trovafloxacin increased serum levels of alanine amino transferases (ALT) and pro-inflammatory cytokines when administered in combination with lipopolysaccharide (LPS) or TNF to mice induces severe liver toxicity associated with vast apoptotic areas in the liver.

Key Properties

• CAS Number: 147059-72-1
• MW: 416.35
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₅F₃N₄O₃
• 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
• Target: DNA gyrase
• Solubility: In Vitro: DMSO : 10 mg/mL (24.02 mM)

Bioactivity

• 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. 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. Animal model: Male C57BL/6 J mice (9-11-week-old) injected with recombinant murine TNF ion. Dosage: 150 mg/kg. Administration: Oral administration. Result: Showed a greater number of cells with increased nuclear/cytoplasmic p65 ratio in liver.
• 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. Trovafloxacin (20 μM; 24 hours; HepG2 cells) and TNF (4 ng/mL) incubation increases expression of early NF-κB-related factors A20 and IκBα. Trovafloxacin prolongs TNF-induced activation of MAPKs and IKKα/β activation in HepG2.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. 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. Apoptosis Analysis 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 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

DNA gyrase