Trovafloxacin mesylate

Research use only, not for human use.

Trovafloxacin mesylate is an effective and selective inhibitor of pannexin 1 channel (PANX1, IC50 = 4 μM).

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.(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. 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. 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.(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) or TNF to mice. In male C57BL/6 J mice, Trovafloxacin mesylate (150 mg/kg; oral administration) disrupts TNF-induced p65 nuclear translocation. Trovafloxacin mesylate treatment increases expression of early NF-κB-related factors A20 and IκBα.

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Others

Other Targets

COMT; Human Endogenous Metabolite; MAO-A; MAO-B

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147059-75-4

512.5

C21H19F3N4O6S

>98% (HPLC)

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CS(O)(=O)=O.[H][C@@]12CN(C[C@]1([H])[C@H]2N)c1nc2n(cc(C(O)=O)c(=O)c2cc1F)-c1ccc(F)cc1F

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(-20℃)

With Ice Pack

≥ 2 years