Trovafloxacin

产品编号 T13231Cas号 147059-72-1

别名 曲伐沙星

Trovafloxacin 是广谱喹诺酮类抗生素，对革兰氏阳性，革兰氏阴性和厌氧菌有活性。它可阻断 DNA 促旋酶和拓扑异构酶 IV 的活性。它也是口服活性的 Pannexin 1通道选择性抑制剂，对 PANX1内向电流的 IC50为 4 μM。

产品编号 T13231别名 曲伐沙星Cas号 147059-72-1

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生物活性

产品描述	Trovafloxacin is a broad-spectrum quinolone antibiotic with potent activity against Gram-positive.
靶点活性	PANX1:4 μM (IC50)
体外活性	In HepG2 cells, Trovafloxacin (20 μM; 24 hours; ) and tumor necrosis factor (TNF; 4 ng/mL) incubation induces apoptosis and increases leakage of lactate dehydrogenase (LDH)[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 TO-PRO-3 uptake inhibitor by apoptotic cells. Trovafloxacin also inhibits ATP release from apoptotic cells. 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].
体内活性	In male C57BL/6 J mice, TNF-induced p65 nuclear translocation disrupted by Trovafloxacin (150 mg/kg; oral administration). Trovafloxacin treatment increases expression of early NF-κB-related factors A20 and IκBα[1]. Trovafloxacin increased serum levels of alanine amino transferases (ALT) and pro-inflammatory cytokines when administered in combination with lipopolysaccharide (LPS) or TNF to mice induces severe liver toxicity associated with vast apoptotic areas in the liver[1].
别名	曲伐沙星