Trovafloxacin mesylate 是一种广谱喹诺酮类抗生素，对革兰氏阳性，革兰氏阴性和厌氧菌具有有效的活性。Trovafloxacin mesylate 可阻断 DNA 促旋酶 (DNA gyrase) 和拓扑异构酶 IV (topoisomerase IV) 的活性。Trovafloxacin mesylate 也是一种有效的，选择性的，口服活性的 Pannexin 1 通道 (PANX1) 抑制剂，对PANX1内向电流的IC50为 4 μM。Trovafloxacin mesylate 不抑制连接蛋白 43 间隙连接或 PANX2。Trovafloxacin mesylate 通过抑制PANX1导致凋亡细胞碎片失调。
| 生物活性 | Trovafloxacin mesylate is a broad-spectrum quinoloneantibioticwith potent activity againstGram-positive,Gram-negativeandanaerobic organisms. Trovafloxacin mesylate blocks theDNA gyraseandtopoisomeraseIVactivity. Trovafloxacin mesylate is also a potent, selective and orally activepannexin 1 channel (PANX1)inhibitor with anIC50of 4 μM forPANX1inward current. Trovafloxacin mesylate does not inhibit connexin 43 gap junction or PANX2. Trovafloxacin mesylate leads to dysregulated fragmentation of apoptotic cells by inhibitingPANX1[1][2][3]. |
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体外研究
(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[1].
Trovafloxacin (20 μM; 24 hours; HepG2 cells) and TNF (4 ng/mL) incubation increases expression of early NF-κB-related factors A20 and IκBα[1].
Trovafloxacin prolongs TNF-induced activation of MAPKs and IKKα/β activation in HepG2[1].
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[2].
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[3].
Apoptosis Analysis[1] | 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[1] | 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. |
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体内研究
(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[1].
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[1].
| Animal Model: | Male C57BL/6 J mice (9-11-week-old) injected with recombinant murine TNF ion[1] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(243.92 mM;ultrasonic and warming and heat to 60℃) H2O : 20 mg/mL(39.03 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9514 mL | 9.7569 mL | 19.5137 mL | | 5 mM | 0.3903 mL | 1.9514 mL | 3.9027 mL | | 10 mM | 0.1951 mL | 0.9757 mL | 1.9514 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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