Moxifloxacin HCl是一种第四代、具有广谱抗菌活性的8-甲氧基氟喹诺酮类抗菌药。
Cas No.:186826-86-8
Sample solution is provided at 25 µL, 10mM.
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Moxifloxacin HCl is a fourth-generation, broad-spectrum 8-methoxyfluoroquinolone antibacterial agent. Moxifloxacin HCl inhibits the activity of bacterial DNA topoisomerase II (DNA gyrase) and topoisomerase IV, thereby blocking bacterial DNA replication and transcription processes, ultimately leading to bacterial death. Moxifloxacin HCl can be used in research related to respiratory tract infections, skin and skin structure infections, intra-abdominal infections, and tuberculosis (especially drug-resistant tuberculosis)[1-4].
In vitro, Moxifloxacin HCl (5-50μg/ml) was co-treated with TNF-α (50ng/ml) in cystic fibrosis bronchial epithelial cell lines IB3 and C38 cells for 48 hours. Moxifloxacin HCl significantly inhibited the secretion of IL-8 and IL-6; Moxifloxacin HCl (5-20μg/ml) was co-treated with TNF-α (50ng/ml) in IB3 and C38 cells for 15-60 minutes. Moxifloxacin HCl significantly inhibited the activation of ERK1/2, JNK, and NF-κB[5]. Moxifloxacin HCl (0.05-1mg/ml) was used to treat immortalized human corneal endothelial cells (B4G12 cells) for 24-72 hours. Moxifloxacin HCl induced dose-dependent cytotoxicity, increased reactive oxygen species generation and autophagy, activated caspase 2, 3, 8 pathways and induced apoptosis[6].
In vivo, Moxifloxacin HCl (12.5, 25, 50mg/kg; once daily) was orally administered to Wistar mice for 7 days. Moxifloxacin HCl significantly increased serum creatinine, cholesterol, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, triglyceride, urea levels and aspartate transaminase, alanine transaminase, alkaline phosphatase activities, while decreasing total bilirubin levels in mice[7]. Moxifloxacin HCl (100mg/kg; twice daily) was intraperitoneally injected into C57BL/6N mice for 2 days. Moxifloxacin HCl significantly reduced the numbers and concentrations of total immune cells, neutrophils, and inflammatory mediators (KC, IL-1β, IL-17A) in the lungs after infection with live or heat-killed bacteria[8].
References:
[1] Balfour JA, Wiseman LR. Moxifloxacin HCl. Drugs. 1999 Mar;57(3):363-73; discussion 374.
[2] Al Omari MM, Jaafari DS, Al-Sou'od KA, Badwan AA. Moxifloxacin HCl hydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:299-431.
[3] Miravitlles M, Anzueto A. Moxifloxacin HCl: a respiratory fluoroquinolone. Expert Opin Pharmacother. 2008 Jul;9(10):1755-72.
[4] Khan F, Ismail M, Khan Q, et al. Moxifloxacin HCl-induced QT interval prolongation and torsades de pointes: a narrative review. Expert Opin Drug Saf. 2018 Oct;17(10):1029-1039.
[5] Blau H, Klein K, Shalit I, et al. Moxifloxacin HCl but not ciprofloxacin or azithromycin selectively inhibits IL-8, IL-6, ERK1/2, JNK, and NF-kappaB activation in a cystic fibrosis epithelial cell line. Am J Physiol Lung Cell Mol Physiol. 2007 Jan;292(1):L343-52.
[6] Park JH, Kim M, Chuck RS, et al. Evaluation of Moxifloxacin HCl-induced cytotoxicity on human corneal endothelial cells. Sci Rep. 2021 Mar 18;11(1):6250.
[7] Ukpo GE, Ebuehi OA, Kareem AA. Evaluation of Moxifloxacin HCl-induced Biochemical Changes in Mice. Indian J Pharm Sci. 2012 Sep;74(5):454-7.
[8] Beisswenger C, Honecker A, Kamyschnikow A, et al. Moxifloxacin HCl modulates inflammation during murine pneumonia. Respir Res. 2014 Jul 17;15(1):82.
Moxifloxacin HCl是一种第四代、具有广谱抗菌活性的8-甲氧基氟喹诺酮类抗菌药。Moxifloxacin HCl通过抑制细菌DNA拓扑异构酶Ⅱ（DNA旋转酶）和拓扑异构酶Ⅳ的活性，阻断细菌DNA复制与转录过程，最终导致细菌死亡。Moxifloxacin HCl可用于呼吸道感染、皮肤及皮肤结构感染、腹腔内感染以及结核病（尤其是耐药结核病）的相关研究[1-4]。
在体外，Moxifloxacin HCl（5-50μg/ml）与TNF-α（50ng/ml）同时处理囊性纤维化支气管上皮细胞系IB3和C38细胞48小时。Moxifloxacin HCl显著抑制IL-8和IL-6的分泌；Moxifloxacin HCl（5-20μg/ml）与TNF-α（50ng/ml）同时处理IB3和C38细胞15-60分钟。Moxifloxacin HCl显著抑制ERK1/2、JNK和NF-κB的激活[5]。Moxifloxacin HCl（0.05-1mg/ml）处理永生化人角膜内皮细胞（B4G12细胞）24-72小时。Moxifloxacin HCl产生剂量依赖性的细胞毒性，增加活性氧生成和自噬，激活caspase 2、3、8通路并诱导细胞凋亡[6]。
在体内，Moxifloxacin HCl（12.5、25、50mg/kg；每日一次）口服给药于Wistar小鼠，连续7天。Moxifloxacin HCl显著增加了小鼠的血清肌酐、胆固醇、高密度脂蛋白胆固醇、低密度脂蛋白胆固醇、甘油三酯、尿素水平以及天冬氨酸转氨酶、丙氨酸转氨酶、碱性磷酸酶活性，同时降低了总胆红素水平[7]。Moxifloxacin HCl（100mg/kg；每天两次）腹腔注射于C57BL/6N小鼠，连续两天。Moxifloxacin HCl显著减少了感染活菌或热灭活细菌后肺部总免疫细胞、中性粒细胞以及炎症介质（KC、IL-1β、IL-17A）的数量和浓度[8]。
| Cell experiment [1]: | |
Cell lines | Immortalized human corneal endothelial cells (B4G12 cell line) |
Preparation Method | B4G12 cells were cultured in human endothelial serum-free medium supplemented with 10ng/ml fibroblast growth factor-2. The cells were treated with various concentrations of Moxifloxacin HCl (0.05-1mg/ml) for 24, 48, and 72 hours. |
Reaction Conditions | 0.05-1mg/ml; 24-72h |
Applications | Moxifloxacin HCl induced dose-dependent cytotoxicity in HCECs. Moxifloxacin HCl exposure increased reactive oxygen species (ROS) generation and induced autophagy in HCECs. Moxifloxacin HCl exposure resulted in significant dose-dependent increases of caspase 2, 3, and 8 activation and induced apoptosis in HCECs. |
| Animal experiment [2]: | |
Animal models | Wistar mice (weighing 17.5-19.0g) |
Preparation Method | Mice were divided into four groups. Group A served as the control and received 2ml of distilled water, while Groups B, C and D were orally administered Moxifloxacin HCl at doses of 12.5, 25 and 50mg/kg body weight once daily for 7 days, respectively. |
Dosage form | 12.5, 25, 50mg/kg; p.o.; once daily for 7 days |
Applications | Moxifloxacin HCl administration significantly increased serum creatinine, cholesterol, high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, triglyceride, urea levels and aspartate transaminase, alanine transaminase, alkaline phosphatase activities, while decreasing total bilirubin levels in a dose-dependent manner. |
References: | |
| Cas No. | 186826-86-8 | SDF | |
| 别名 | 莫西沙星盐酸盐; BAY 12-8039 | ||
| 化学名 | 7-[(4aS,7aS)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxoquinoline-3-carboxylic acid;hydrochloride | ||
| Canonical SMILES | COC1=C2C(=CC(=C1N3CC4CCCNC4C3)F)C(=O)C(=CN2C5CC5)C(=O)O.Cl | ||
| 分子式 | C21H24FN3O4.HCl | 分子量 | 437.89 |
| 溶解度 | ≥ 19.15mg/mL in DMSO, ≥ 25.4mg/mL in Water with gentle warming | 储存条件 | 4°C, protect from light |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2837 mL | 11.4184 mL | 22.8368 mL |
| 5 mM | 456.7 μL | 2.2837 mL | 4.5674 mL |
| 10 mM | 228.4 μL | 1.1418 mL | 2.2837 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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