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曲伐沙星甲磺酸盐

曲伐沙星甲磺酸盐

英文名称:Trovafloxacin Mesylate
CAS号:147059-75-4
分子式:C21H19F3N4O6S
分子量:512.46
EINECS号:
Mol文件:147059-75-4.mol
曲伐沙星甲磺酸盐 结构式

曲伐沙星甲磺酸盐 性质

熔点 >250°C (dec.)
储存条件 room temp
溶解度 二甲基亚砜:>10mg/mL
形态 粉末
颜色 白色至类白色

曲伐沙星甲磺酸盐 用途与合成方法

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。

IC50: 4 μM (Pannexin 1 channel (PANX1))
Gram-positive, Gram-negative and anaerobic organisms
DNA gyrase
Topoisomerase IV

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.

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.

安全信息

危险品标志C
危险类别码63-34
安全说明26-36-45
危险品运输编号UN 1759 8 / PGIII
WGK Germany3
RTECS号QN2791250
毒性women,LDLo,oral,2mg/kg (2mg/kg),SKIN AND APPENDAGES (SKIN): "DERMATITIS, OTHER: AFTER SYSTEMIC EXPOSURE",Archives of Internal Medicine. Vol. 159, Pg. 2225, 1999.

曲伐沙星甲磺酸盐 上下游产品信息

曲伐沙星甲磺酸盐供应商 更多

华阴市赛普生物科技有限公司
黄金产品 现货
联系电话: 13892502238
产品介绍:
中文名称:曲伐沙星甲磺酸盐
英文名称:Trovafloxacin mesylate
CAS:147059-75-4
纯度:95+
包装信息:1g
备注:15g
库存量:>10g
现货日期:2024/12/2 13:17:10
威尔曼医药集团有限公司
现货
联系电话:027-027-83778875 15807197853
产品介绍:
中文名称:甲磺酸曲伐沙星
英文名称:Trovafloxacin Mesylate
CAS:147059-75-4
包装信息:1g/RMB 5800;10g/RMB 46000
备注:下单后顺丰快递发货,网络实时追踪,3天及时送货上门, 1G/瓶 98% 现货价格钜惠 98% HPLC 总价5800
库存量:458g
现货日期:2024/11/21 14:03:56
北京百灵威科技有限公司
联系电话:010-82848833 400-666-7788
产品介绍:
中文名称:曲伐沙星甲磺酸
英文名称:Trovafloxacin Mesylate
CAS:147059-75-4
包装信息:100Mg,10Mg
备注:化学试剂、精细化学品、医药中间体、材料中间体
武汉易泰科技有限公司上海分公司
联系电话:821-50328103-801 18930552037
产品介绍:
英文名称:Trovafloxacin Mesylate;7-[(1α,5α,6α)-6-AMino-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylicacidMesylate
CAS:147059-75-4
纯度:99% HPLC
包装信息:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
武汉丰泰威远科技有限公司
联系电话:027-87465837 19945049750
产品介绍:
中文名称:甲磺酸曲伐沙星
英文名称:Trovafloxacin Mesylate
CAS:147059-75-4
纯度:97.0%
包装信息:1g;10g;25g;500g;1kg
备注:试剂级

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