147059-72-1 曲伐沙星

中文名称: 曲伐沙星
英文名称: TROVAFLOXACIN
CAS号
分子式

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名称和标识

中文名: 曲伐沙星
英文名: TROVAFLOXACIN
CAS号: 147059-72-1
分子式: C20H15F3N4O3
分子量: 416.36
中文别名: 特伐沙星; (1Α,5Α,6Α)-7-(6-氨基-3-氮杂二环[3.1.0]己-3-基)-1-(2,4-二氟苯基)-6-氟-1,4-二氢-4-氧-1,8-萘啶-3-羧酸; 曲氟沙星
英文别名: 1,8-Naphthyridine-3-carboxylic acid, 7-(1.alpha.,5.alpha.,6.alpha.)-6-amino-3-azabicyclo3.1.0hex-3-yl-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-; (1α,5α,6α)-7-(6-Amino-3-azabi-cyclo[3.1.0]hex-3-y1)-1-(2,4-difluomphenyl)-6-fluom-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid; CP-99219; 7-[(1R,5S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-keto-1,8-naphthyridine-3-carboxylic acid; 7-[(1R,5S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid; 7-[(1R,5S)-6-azanyl-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid

物化属性

储存条件: -20°C Freezer, Under inert atmosphere
外观: 淡米色至浅米色
密度: 1.612±0.06 g/cm³
形态: 固体
溶解度: 可溶于乙腈（少许）、DMSO（少许）
熔点

生产及用途

用途与制备

生物活性 Trovafloxacin 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 可阻断 DNA 促旋酶 (DNA gyrase) 和拓扑异构酶 IV (topoisomerase IV) 的活性。Trovafloxacin 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 不抑制 connexin 43 gap junction 或 PANX2。Trovafloxacin 通过抑制 PANX1 导致凋亡细胞碎片失调。
靶点 IC50: 4 μM (Pannexin 1 channel (PANX1)) Gram-positive, Gram-negative and anaerobic organisms DNA gyrase Topoisomerase IV
体外研究 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 Incubation Time: 24 hours Result: Caused a higher increase in the transcription of A20 and IκBα in HepG2 cells.

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