Trovafloxacin mesylate 是一种有效的特异性 pannexin 1 通道抑制剂 (PANX1, IC50 = 4 μM)。Trovafloxacin mesylate 对革兰氏阳性、革兰氏阴性和厌氧菌具有强效活性。 Trovafloxacin mesylate 阻断 DNA 促旋酶和拓扑异构酶 IV 活性。

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.

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].

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

147059-75-4

C21H19F3N4O6S

512.46

DMSO:120 mg/mL (234.16 mM),ultrasonic and warming and heat to 60°C
H2O:18 mg/mL (35.12 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years