Flumequine(Synonyms: 氟甲喹; R-802)

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Flumequine (Synonyms: 氟甲喹; R-802) 纯度: 99.44%

Flumequine (R-802) 是一种喹诺酮类抗生素，为拓扑异构酶 II (Topoisomerase II) 抑制剂，IC50 值为 15 μM (3.92 μg/mL)。

Flumequine(Synonyms: 氟甲喹; R-802)

Flumequine Chemical Structure

CAS No. : 42835-25-6

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生物活性

Flumequine (R-802) is a quinolone antibiotic, and acts as a topoisomerase II inhibitor, with an IC50 of 15 μM (3.92 μg/mL).

IC50 & Target

Topoisomerase II

15 μM (IC50)

体外研究
(In Vitro)

Flumequine (R-802) is a topoisomerase II inhibitor, with an IC50 of 3.92 μg/mL, and less potently inhibits Gyrase, with an IC50 of 1764 μg/mL. Flumequine (0-625 μg/mL) increases migration of nuclear DNA from CHL cells[1]. Flumequine (R-802) inhibits Spanish field isolates of B. hyodysenteriae with MIC50 and MIC90 of 50 and 100 μg/mL, and MBC50 and MBC90 of 50, 200 μg/mL, respectively[2]. Flumequine (R-802) suppresses A. salmonicida isolates with MIC ranging from 0.06 to 32 μg/mL[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Flumequine (R-802) (0-500 mg/kg, p.o.) causes dose-related DNA damage in the stomach, colon, and urinary bladder of mice, 1 and 3 h but not 24 h after its administration[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

261.25

Formula

C14H12FNO3
CAS 号

42835-25-6
中文名称

氟甲喹；氟灭菌
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
溶解性数据
In Vitro: 

DMSO : 7.69 mg/mL (29.44 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.8278 mL 19.1388 mL 38.2775 mL
5 mM 0.7656 mL 3.8278 mL 7.6555 mL
10 mM 0.3828 mL 1.9139 mL 3.8278 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°C, 6 months; -20°C, 1 month。-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。
参考文献

  • [1]. Kashida Y, et al. Mechanistic study on flumequine hepatocarcinogenicity focusing on DNA damage in mice. Toxicol Sci. 2002 Oct;69(2):317-21.

    [2]. Aller-Morán LM, et al. Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriae. Res Vet Sci. 2015 Dec;103:51-3.

    [3]. Giraud E, et al. Mechanisms of quinolone resistance and clonal relationship among Aeromonas salmonicida strains isolated from reared fish with furunculosis. J Med Microbiol. 2004 Sep;53(Pt 9):895-901.
Cell Assay
[1]

The Chinese hamster lung cell line CHL/IU is routinely maintained in monolayer culture in Dulbecco’s modified MEM medium supplemented with 10% fetal bovine serum at 37°C under a 5% CO2 atmosphere. Exponentially growing cells are treated with Flumequine (R-802) dissolved in DMSO for 1 h. The dose range is chosen in order to obtain both damaged and highly damaged cells. Following Flumequine (R-802) treatment, cells are embedded in GP42 agarose dissolved in saline at 1%. Cell number and cell viability are determined for each dose[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Infant and young-adult male ddY mice at 4 and 7 weeks of age, respectively, are used after 1 week of acclimatization. Groups are treated once orally with Flumequine (R-802) at <500 mg>. Adult mice are sacrificed at 3 and 24 h after treatment, and 8 organs, the stomach, colon, liver, kidney, urinary bladder, lung, brain, and bone marrow, are removed. Infant mice are sacrificed 3 and 24 h after treatment, and the livers are excised. In another study, the genotoxicity of Flumequine (R-802) is studied in the regenerating liver of adult mice. For this purpose, male mice at 8 weeks-of-age are anesthetized with ether and 3 major lobes of the liver, left lateral lobe, left medial lobe, and right lateral lobe, are removed. Four days after the hepatectomy, mice are subjected to oral administration of Flumequine (R-802) once. They are sacrificed 3 h after FL-treatment and regenerated livers are sampled. Slides for the comet assay are prepared at each set time[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Kashida Y, et al. Mechanistic study on flumequine hepatocarcinogenicity focusing on DNA damage in mice. Toxicol Sci. 2002 Oct;69(2):317-21.

    [2]. Aller-Morán LM, et al. Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriae. Res Vet Sci. 2015 Dec;103:51-3.

    [3]. Giraud E, et al. Mechanisms of quinolone resistance and clonal relationship among Aeromonas salmonicida strains isolated from reared fish with furunculosis. J Med Microbiol. 2004 Sep;53(Pt 9):895-901.

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