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Trovafloxacin mesylate

Catalog No. T13231L CAS 147059-75-4

Trovafloxacin mesylate is an effective and selective inhibitor of pannexin 1 channel (PANX1, IC50 = 4 μM). Trovafloxacin mesylate exhibits potent activity against Gram-positive, Gram-negative, and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and Topoisomerase IV activity.

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Trovafloxacin mesylate, CAS 147059-75-4

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Trovafloxacin mesylate is an effective and selective inhibitor of pannexin 1 channel (PANX1, IC50 = 4 μM). Trovafloxacin mesylate exhibits potent activity against Gram-positive, Gram-negative, and anaerobic organisms. Trovafloxacin mesylate blocks the DNA gyrase and topoisomerase IV activity.
Targets&IC50	Pannexin 1 channel (PANX1):4 μM
In vitro	Trovafloxacin mesylate is an inhibitor of TO-PRO-3 uptake by apoptotic cells and inhibits ATP release from apoptotic cells. Trovafloxacin mesylate does not inhibit caspase 3/7 activation, or caspase-mediated PANX1 cleavage during apoptosis[1]. Trovafloxacin mesylate 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 mesylate at which 90% of isolates are inhibited for 55 isolates of pneumococci is 0.125 μg/mL[2]. Trovafloxacin mesylate prolongs TNF-induced activation of MAPKs and IKKα/β activation in HepG2 cells. Trovafloxacin mesylate (20 µM; 24 hours) and tumor necrosis factor (TNF; 4 ng/mL) incubation induces apoptosis and increases leakage of lactate dehydrogenase (LDH). Trovafloxacin mesylate (20 µM; 24 hours) and TNF (4 ng/mL) incubation increases expression of early NF-κB-related factors A20 and IκBα[3].
In vivo	Trovafloxacin mesylate induces severe liver toxicity associated with vast apoptotic areas in the liver, increased serum levels of alanine amino transferases (ALT) and pro-inflammatory cytokines when administered in combination with lipopolysaccharide (LPS

Molecular Weight	512.46
Formula	C21H19F3N4O6S
CAS No.	147059-75-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 120 mg/mL (234.16 mM), ultrasonic and warming and heat to 60°C

H2O: 18 mg/mL (35.12 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Poon IK, et al. Unexpected link between an antibiotic, pannexin channels and apoptosis. Nature. 2014 Mar 20;507(7492):329-34. 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. 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.

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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.

Keywords

Trovafloxacin mesylate 147059-75-4 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology Others DNA/RNA Synthesis Topoisomerase Antibacterial topoisomerase-IV TNF gyrase Bacterial hepatotoxicity LPS Trovafloxacin broad-spectrum Antibiotic DNA Inhibitor PANX1 pneumococci inhibit pro-inflammatory NF-κB inhibitor

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