Temafloxacin (TMFX) 是一种口服有效的喹诺酮类广谱抗菌剂。Temafloxacin 对下呼吸道和泌尿生殖道感染具有较好的耐受性。
| 生物活性 | Temafloxacin (TMFX) is an orally activequinolonebroad-spectrum antibacterial agent. Temafloxacin is well tolerated in lower respiratory and genitourinary tract infections[1][2]. |
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体外研究
(In Vitro) | Temafloxacin (0-64 μg/mL; 18-24 h) shows good antibacterial activity for gram-positive/negative bacteria, with MIC ranges of<0.004-0.5, 0.5-2 and 0.06-0.25 μg/mL forE. coli,P. aeruginosa, andS. aureus, respectively[1].
Cell Viability Assay[1] | Cell Line: | E. coli(16 strains),P. aeruginosa(13 strains), andS. aureus(17 strains). | | Concentration: | 0-64 μg/mL | | Incubation Time: | 18-24 h | | Result: | InhibitedE. coli(16 strains),P. aeruginosa, andS. aureuswith MIC ranges of<0.004-0.5 (MIC 90%=0.06, =0.06), 0.5-2 (MIC 90%=1, MIC 50%=1) and 0.06-0.25 μg/mL (MIC 90%=0.125, MIC 50%=0.125). MIC 90% and 50% means MIC for 90% and 50% of the isolates (unit: μg/mL). |
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体内研究
(In Vivo) | Temafloxacin (6.25, 25, 100 mg/kg; p.o.; single) shows good inhibitory activity to murine pyelonephritis[1].
Temafloxacin hydrochloride (100 mg/kg; p.o. or s.c.; single) shows rapid gastrointestinal absorption, and has excellent tissue and body fluid penetration and concentration (except for central nervous system (CNS))[1].
| Animal Model: | Female CF-1 mice (20-25 g) (murine pyelonephritis model)[1]. | | Dosage: | 6.25, 25, 100 mg/kg | | Administration: | Orally; single. | | Result: | Reduced the number of viable bacteria in the kidneys of mice. |
| Animal Model: | Female CF-1 mice (20-25 g)[1]. | | Dosage: | 100 mg/kg | | Administration: | Subcutaneously or orally; single. | | Result: | 1.19Pharmacokinetic Parameters of Temafloxacin hydrochloride in Female CF-1 mice[1].
| Cmax(μg/mL) | AUC (μg/mLoh) | T1/2(h) | % Urinary recovery | | SC (100 mg/kg) | 25.2 | 86.6 | 3.4 | 25.3 | | PO (100 mg/kg) | 13.5 | 57.4 | 1.3 | 9.1 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO :< 1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble or slightly soluble) 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 90%corn oil Solubility: ≥ 0.5 mg/mL (1.20 mM); Clear solution
此方案可获得 ≥ 0.5 mg/mL (1.20 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 5.0 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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