Orbifloxacin是一种合成的氟喹诺酮类药物，具有广谱杀菌活性。
Cas No.:113617-63-3
Sample solution is provided at 25 µL, 10mM.
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Orbifloxacin is a synthetic fluoroquinolone with broad spectrum bactericidal activity [1]. Orbifloxacin exerts bactericidal activity by inhibiting bacterial DNA gyrase and topoisomerase IV, thereby disrupting DNA replication and bacterial proliferation [2]. Orbifloxacin accumulates in leukocytes, which allows it to act on intracellular bacteria and be transported to and liberated at the sites of infection [3]. Orbifloxacin is widely used for the treatment of gastrointestinal and respiratory infections in cattle and swine[4].
In vivo, Orbifloxacin treatment via intramuscular injection at a single dose of 20mg/kg can effectively inhibit the bacterial load of Staphylococcus aureus ATCC 29213 in a neutropenic murine thigh infection model within 24 hours[5].
References:
[1] Santos O M M, Freitas J T J, Bitencourt M, et al. Three new orbifloxacin multicomponent crystal forms towards pharmaceutical improvement[J]. Journal of Molecular Structure, 2020, 1217: 128371.
[2] D’Atanasio N, Capezzone de Joannon A, Di Sante L, et al. Antibacterial activity of novel dual bacterial DNA type II topoisomerase inhibitors[J]. PLoS One, 2020, 15(2): e0228509.
[3] Scott D W, Peters J, Miller Jr W H. Efficacy of orbifloxacin tablets for the treatment of superficial and deep pyoderma due to Staphylococcus intermedius infection in dogs[J]. The Canadian Veterinary Journal, 2006, 47(10): 999.
[4] Marín P, Fernandez‐Varon E, Escudero E, et al. Pharmacokinetic–pharmacodynamic integration of orbifloxacin in rabbits after intravenous, subcutaneous and intramuscular administration[J]. Journal of veterinary pharmacology and therapeutics, 2008, 31(1): 77-82.
[5] Zhong L G, Tang S J, Liang L Y, et al. In vivo pharmacokinetic and pharmacodynamic profiles of orbifloxacin against Staphylococcus aureus in a neutropenic murine thigh infection model[J]. BMC Veterinary Research, 2025, 21(1): 531.
Orbifloxacin是一种合成的氟喹诺酮类药物，具有广谱杀菌活性[1]。Orbifloxacin通过抑制细菌DNA旋转酶和拓扑异构酶IV，从而破坏DNA复制和细菌增殖，发挥杀菌活性[2]。Orbifloxacin可在白细胞中积聚，从而作用于细胞内细菌，并被转运至感染部位释放[3]。Orbifloxacin广泛用于治疗牛和猪的胃肠道及呼吸道感染[4]。
在体内，在嗜中性粒细胞减少小鼠大腿感染模型中，单次肌肉注射20mg/kg剂量的Orbifloxacin，可在24小时内有效抑制金黄色葡萄球菌ATCC 29213的细菌载量[5]。
| Animal experiment [1]: | |
Animal models | BALB/c mice |
Preparation Method | Six-week-old, specific-pathogen-free (SPF) BALB/c mice of both sexes (18-20g) were housed in a temperature-controlled (23±2°C) room maintained on a 12/12h light/dark cycle. Neutropenia (neutrophil count; ≤100/mm3) was induced via intraperitoneal injection of cyclophosphamide at 150mg/kg four days and 100mg/kg one day prior to bacterial challenge. Mice were then inoculated with 0.1ml of an early logarithmic-phase S. aureus suspension (106-7 cfu/ml) into the right posterior thigh muscle. Orbifloxacin treatment (20mg/kg; i.m.) was initiated 2h post-infection. After 24h of treatment, mice were euthanized, and the infected thighs were aseptically removed, homogenized, serially diluted, and plated quantification of bacterial burden. |
Dosage form | 20mg/kg for once; i.m. |
Applications | Orbifloxacin treatment inhibited the bacterial load of S. aureus in a neutropenic murine thigh infection model. |
References: | |
| Cas No. | 113617-63-3 | SDF | |
| 别名 | 奥比沙星; CP-104354 | ||
| 化学名 | 1-cyclopropyl-7-[(3S,5R)-3,5-dimethylpiperazin-1-yl]-5,6,8-trifluoro-4-oxoquinoline-3-carboxylic acid | ||
| Canonical SMILES | CC1CN(CC(N1)C)C2=C(C3=C(C(=C2F)F)C(=O)C(=CN3C4CC4)C(=O)O)F | ||
| 分子式 | C19H20F3N3O3 | 分子量 | 395.38 |
| 溶解度 | ≥ 6.7mg/mL in DMSO with gentle warming | 储存条件 | Store at 4°C |
| 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 | 2.5292 mL | 12.6461 mL | 25.2921 mL |
| 5 mM | 505.8 μL | 2.5292 mL | 5.0584 mL |
| 10 mM | 252.9 μL | 1.2646 mL | 2.5292 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet