Clinafloxacin (AM 1091) 是一种高效广谱氟喹诺酮类抗生素 (antibiotic)，对革兰氏阳性、革兰氏阴性和厌氧病原体均有抑制活性。Clinafloxacin 对金黄色葡萄球菌的 DNA 促旋酶 (DNA gyrase) 和拓扑异构酶 IV (topoisomerase IV) 有抑制作用，IC50值分别为 0.92 μg/ml 和 1.62 μg/ml。
| 生物活性 | Clinafloxacin (AM 1091) is a potent and broad-spectrum fluoroquinoloneantibiotic, has inhibitory activity against gram-positive, gram-negative bacterias, and anaerobic pathogens in vitro[1]. Clinafloxacin is againstDNA gyraseandtopoisomeraseIVof S. aureuswithIC50values of 0.92 μg/ml and 1.62 μg/ml, respectively[2]. |
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体外研究
(In Vitro) | Clinafloxacin exhibits activity againstS. pneumoniawith anMICof 1μg/ml for the parC-gyrA mutants[2].
Clinafloxacin hydrochloride has antibacterial activities against target-altered mutant strains of S. aureus. It against Wild typeS. aureus,gyrA mutantS. aureusandgyrA mutantS. aureuswith MIC values of 0.016 μg/ml, 0.063 μg/ml and 0.915 μg/ml, respectively[3].
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体内研究
(In Vivo) | Clinafloxacin is very effective for the therapy of penicillin-resistant, ciprofloxacin-susceptible pneumococcal meningitis in the rabbit model.
With the CS strain (2349)(Clinafloxacin MIC=0.12 μg/ml), at a dose of 10 mg/kg and 20 mg/kg per day Clinafloxacin achieves an initial reduction at 6 hr. Both are bactericidal at this point but presents regrowth at 24 hr, and the final reduction at 24 hr in mean log cfu/ml is 22.30 and 23.83, respectively. However, With the CR strain (4371)(Clinafloxacin MIC=0.5 μg/ml), Clinafloxacin even at 20 mg/kg per day does not decrease bacterial titers at any time point in this rabbit model of meningitis[3].
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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 : 2 mg/mL(5.47 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 2.7338 mL | 13.6690 mL | 27.3381 mL | | 5 mM | 0.5468 mL | 2.7338 mL | 5.4676 mL | | 10 mM | --- | --- | --- |
*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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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