Tosufloxacin (A-61827) tosylate hydrate 是一种具有口服活性的氟喹诺酮类抗生素。Tosufloxacin 对革兰氏阳性和革兰氏阴性细菌表现出广泛的抗菌活性。
| 生物活性 | Tosufloxacin tosylate hydrate (A-61827) is an orally active fluoroquinoloneantibiotic. Tosufloxacin shows a broad spectrum of antibacterial activity against gram-positive and gram-negative bacteria[1][2]. |
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体外研究
(In Vitro) | Tosufloxacin tosylate hydrate (T-3262) (0.05-3.13 μg/mL; 18 h) shows antibacterial activities againstS. aureus,Staphylococcus epidermidis,streptococci,enterococci,Bacteroides fragilis,Clostridium difficile, andClostridium perfringens[2].
Cell Viability Assay[2] | Cell Line: | S. aureus,Staphylococcus epidermidis,streptococci,enterococci,Bacteroides fragilis,Clostridium difficile, andClostridium perfringens | | Concentration: | 0.05-3.13 μg/mL | | Incubation Time: | 18 hours | | Result: | Showed MIC90s (MICs for 90% of the isolates tested) ranging from 0.05 to 1.56 μg/mL forS. aureus,Staphylococcus epidermidis,streptococci, andenterococci.
Showed MIC90s of 1.56, 3.13, and 0.20 μg/mL forBacteroides fragilis,Clostridium difficile, andClostridium perfringens, respectively. |
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体内研究
(In Vivo) | Tosufloxacin tosylate hydrate (T-3262) (oral gavage; 0.16-13.39 mg/kg; once) treatment shows antibacterial activity againstS. aureus,E. coli, andP. aeruginosain vivo[2].
| Animal Model: | Male Slc:ICR mice infected withS. aureus[2] | | Dosage: | 1.27-2.15 mg/kg | | Administration: | Oral gavage; 1.27-2.15 mg/kg; once | | Result: | Showed 50% effective dose (ED50) of 1.62 mg/kg (body weight) at 7 days after infection.
Showed MIC value of 0.0125 μg/mL. |
| Animal Model: | Male Slc:ICR mice infected withE. coli[2] | | Dosage: | 0.16-0.30 mg/kg | | Administration: | Oral gavage; 0.16-0.30 mg/kg; once | | Result: | Showed 50% effective dose (ED50) of 0.22 mg/kg (body weight) at 7 days after infection.
Showed MIC value of 0.0125 μg/mL. |
| Animal Model: | Male Slc:ICR mice infected withP. aeruginosa[2] | | Dosage: | 7.66-13.39 mg/kg | | Administration: | Oral gavage; 7.66-13.39 mg/kg; once | | Result: | Showed 50% effective dose (ED50) of 10.13 mg/kg (body weight) at 7 days after infection.
Showed MIC value of 0.78 μg/mL. |
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| 结构分类 | - Antibiotics
- Other Antibiotics
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 12.5 mg/mL(21.02 mM;Need ultrasonic) H2O : 1 mg/mL(1.68 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 1.6819 mL | 8.4096 mL | 16.8192 mL | | 5 mM | 0.3364 mL | 1.6819 mL | 3.3638 mL | | 10 mM | 0.1682 mL | 0.8410 mL | 1.6819 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 1.25 mg/mL (2.10 mM); Suspended solution; Need ultrasonic
此方案可获得 1.25 mg/mL (2.10 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.25 mg/mL (2.10 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (2.10 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1.25 mg/mL (2.10 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (2.10 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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