Flumequine是一种生物利用度良好的氟喹诺酮类抗生素，也是拓扑异构酶II的抑制剂，IC50值为15μM。
Cas No.:42835-25-6
Sample solution is provided at 25 µL, 10mM.
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Flumequine is a fluoroquinolone antibiotic with favorable bioavailability and acts as an inhibitor of topoisomerase II, with an IC50 value of 15μM[1,2]. Flumequine exerts its antibacterial effect by inhibiting bacterial DNA gyrase, thereby blocking DNA replication[3], and is commonly used in the treatment of intestinal infections in livestock and fish[4,5].
In vitro, treatment of B16F10 mouse melanoma cells with Flumequine (12.5, 25, 50μM) for 72h increased extracellular melanin content by 6.1 ± 1.6%, 9.4 ± 0.5%, and 11.6 ± 0.3%, respectively, and intracellular melanin content by 42.2 ± 3.6%, 58.1 ± 1.0%, and 59.1 ± 0.6%, respectively. Treatment with Flumequine (50μM) for 48h significantly upregulated the mRNA expression levels of microphthalmia-associated transcription factor (MITF) and tyrosinase in B16F10 cells[6].
In vivo, oral administration of Flumequine (750mg/kg; once daily) to pubertal male Wistar rats for six weeks significantly reduced serum levels of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), and interferon-γ (IFN-γ). From day 7 of treatment onward, body weight gain was significantly slowed, and the relative weights of the brain, adrenal glands, thyroid gland, and testes were significantly increased[7]. In rainbow trout infected with red mouth disease, oral administration of Flumequine (12mg/kg/day) via medicated feed for 8 days resulted in a significant increase in the proportion of Flumequine-resistant Aeromonas spp. on the skin and in the gut contents of the fish at 24h post-treatment[8].
References:
[1] GIGUÈRE S, DOWLING P M. Fluoroquinolones[J]. Antimicrobial therapy in veterinary medicine, 2013: 295-314.
[2] KASHIDA Y, SASAKI Y F, OHSAWA K, et al. Mechanistic study on flumequine hepatocarcinogenicity focusing on DNA damage in mice[J]. Toxicological Sciences, 2002, 69(2): 317-321.
[3] ALDRED K J, KERNS R J, OSHEROFF N. Mechanism of quinolone action and resistance[J]. Biochemistry, 2014, 53(10): 1565-1574.
[4] RODRÍGUEZ J M, DIEZ M J, SIERRA M, et al. Distribution of flumequine in intestinal contents and colon tissue in pigs after its therapeutic use in the drinking water[J]. Animals, 2021, 11(6): 1514.
[5] TOURAKI M, NIOPAS I, LADOUKAKIS E, et al. Efficacy of flumequine administered by bath or through medicated nauplii of Artemia fransiscana (L.) in the treatment of vibriosis in sea bass larvae[J]. Aquaculture, 2010, 306(1-4): 146-152.
[6] KARUNARATHNE W A H M, MOLAGODA I M N, KIM M S, et al. Flumequine-mediated upregulation of p38 MAPK and JNK results in melanogenesis in B16F10 cells and zebrafish larvae[J]. Biomolecules, 2019, 9(10): 596.
[7] KANG J W, HOSSAIN M A, CHOI B, et al. Toxicological evaluation of flumequine in pubertal male rats after oral administration for six weeks[J]. Journal of Veterinary Research, 2018, 62(1): 87.
[8] NAVINER M, GORDON L, GIRAUD E, et al. Antimicrobial resistance of Aeromonas spp. isolated from the growth pond to the commercial product in a rainbow trout farm following a flumequine treatment[J]. Aquaculture, 2011, 315(3-4): 236-241.
Flumequine是一种生物利用度良好的氟喹诺酮类抗生素，也是拓扑异构酶II的抑制剂，IC50值为15μM[1,2]。Flumequine通过抑制细菌DNA回旋酶以阻止DNA复制发挥作用[3]，通常用于家畜和鱼类肠道疾病的治疗和研究[4,5]。
在体外，Flumequine（12.5, 25, 50μM）处理小鼠黑色素瘤B16F10细胞72h，细胞外黑色素含量分别增加6.1 ± 1.6%、9.4 ± 0.5%和11.6 ± 0.3%，细胞内黑色素含量分别增加42.2 ± 3.6%、58.1 ± 1.0%和59.1 ± 0.6%。Flumequine（50μM）处理B16F10细胞48h，显著上调了小眼畸形相关转录因子（MITF）和酪氨酸酶的mRNA表达水平[6]。
在体内，Flumequine（750mg/kg; once daily）口服给予青春期雄性Wistar大鼠6周，血清白细胞介素-6（IL-6）、肿瘤坏死因子-α（TNF-α）和干扰素-γ（IFN-γ）水平显著降低。且从给药第7天起，大鼠体重增长显著减缓，脑、肾上腺、甲状腺和睾丸的相对重量显著增加[7]。Flumequine（12mg/kg/day）通过药饲口服给予感染红嘴病的虹鳟鱼8天，治疗后24h，鱼皮肤和鱼肠道内容物中Flumequine耐药气单胞菌的比例显著升高[8]。
| Cell experiment [1]: | |
Cell lines | B16F10 cells |
Preparation Method | B16F10 cells were cultured at 1×104 cells/mL in 6-well plates overnight and treated with the Flumequine (12.5, 25, 50μM) for 72h. α-MSH (500ng/mL) was used as a positive control. Extracellular melanin content was measured using culture media at 405nm. In order to measure intracellular melanin content, the cells were washed in ice-cold PBS and dissolved in 1M NaOH containing 10% DMSO at 100℃ for 10min. Then, absorbance was measured at 405nm. |
Reaction Conditions | 12.5, 25, and 50μM; 72h |
Applications | Treatment of B16F10 cells with 12.5, 25, and 50μM Flumequine increased extracellular melanin content by 6.1 ± 1.6%, 9.4 ± 0.5%, and 11.6 ± 0.3%, respectively, while increasing intracellular melanin content by 42.2 ± 3.6%, 58.1 ± 1.0%, and 59.1 ± 0.6%, respectively. |
| Animal experiment [2]: | |
Animal models | Pubertal male Wistar rats |
Preparation Method | Pubertal male Wistar rats were orally administered with Flumequine (750mg/kg; once daily) for six weeks. Approximately 24h after the last treatment, blood samples were collected, and serum concentrations of IL-6, TNF-α, and IFN-γ were determined with a Bio-plex rat cytokine-9-plex A panel. |
Dosage form | 750mg/kg; once daily; six weeks; p.o. |
Applications | Treatment of Flumequine significantly reduced the levels of IL-6, TNF-α, and IFN-γ. |
References: | |
| Cas No. | 42835-25-6 | SDF | |
| 别名 | 氟甲喹; R-802 | ||
| 化学名 | 9-fluoro-5-methyl-1-oxo-1,5,6,7-tetrahydropyrido[3,2,1-ij]quinoline-2-carboxylic acid | ||
| Canonical SMILES | FC1=C([H])C2=C(C3=C1[H])N(C([H])=C(C(O[H])=O)C3=O)C(C([H])([H])[H])([H])C([H])([H])C2([H])[H] | ||
| 分子式 | C14H12FNO3 | 分子量 | 261.25 |
| 溶解度 | ≥ 9.35mg/mL in DMSO | 储存条件 | Store at -20°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 | 3.8278 mL | 19.1388 mL | 38.2775 mL |
| 5 mM | 765.6 μL | 3.8278 mL | 7.6555 mL |
| 10 mM | 382.8 μL | 1.9139 mL | 3.8278 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 | ||||||||||
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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。
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