Trovafloxacin mesylate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Trovafloxacin mesylate 是一种有效的选择性 pannexin 1 通道 (PANX1, IC50 = 4 μM) 抑制剂。

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.

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 ncubation Time:24 hours Result:Caused a higher increase in the transcription of A20 and IκBα in HepG2 cells.

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; once Result:Showed a greater number of cells with increased nuclear/cytoplasmic p65 ratio in liver.

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Others

Other Targets

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

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147059-75-4

512.46

C21H19F3N4O6S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (243.92 mM)

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