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My CartCAS：42835-25-6
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 42835-25-6 |
| Name | Flumequine |
| Molecular Formula | C14H12FNO3 |
| Molecular Weight | 261.25 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 255-962-6 |
| MDL | MFCD00079298 |
| SMILES | O=C(C1=CN2C(C)CCC3=C2C(C1=O)=CC(F)=C3)O |
| InChIKey | DPSPPJIUMHPXMA-UHFFFAOYSA-N |
| InChI | InChI=1S/C14H12FNO3/c1-7-2-3-8-4-9(15)5-10-12(8)16(7)6-11(13(10)17)14(18)19/h4-7H,2-3H2,1H3,(H,18,19) |
| PubChem CID | 3374 |
| Target Point | Bacterial;Topoisomerase |
| Passage | DNA Damage/DNA Repair;Anti-infection |
| Background | It is a quinolone antibiotic that is a Topoisomerase II inhibitor. |
| Biological Activity | Flumequine 是一种喹诺酮类抗生素，为Topoisomerase II抑制剂，IC50 值为 15 μM (3.92 μg/mL)[1-3]。 |
| IC50 | Topoisomerase II:15μM [1-3] |
| In Vitro | Flumequine是拓扑异构酶II抑制剂，IC50为3.92μg/ mL，有效抑制Gyrase，IC50为1764μg/ mL。 Flumequine(0-625μg/ mL)可增加CHL细胞核DNA的迁移[1]。 Flumequine抑制西班牙猪痢疾短螺旋体分离株，MIC50和MIC90分别为50和100μg/ mL，MBC50和MBC90分别为50，200μg/ mL [2]。 Flumequine抑制A. salmonicida分离株，MIC范围为0.06至32μg/ mL [3]。 |
| In Vivo | Flumequine(0-500 mg/kg，po)在小鼠的胃，结肠和膀胱中引起剂量相关的DNA损伤，给药后1小时和3小时但不是24小时[1]。 |
| Cell Experiment | 中国仓鼠肺细胞系CHL/IU常规维持在单层培养物中，在Dulbecco改良的MEM培养基中，在37℃，5％CO 2气氛下补充有10％胎牛血清。用溶于DMSO中的Flumequine处理指数生长的细胞1小时。选择剂量范围是为了获得受损和高度受损的细胞。氟喹处理后，将细胞以1％溶解于盐水中的GP42琼脂糖中。确定每种剂量的细胞数和细胞活力[1]。 |
| Animal Experiment | 分别在4周和7周龄的婴儿和年轻成年雄性ddY小鼠在适应环境1周后使用。用氟尿喹以<500mg/kg口服治疗组。处理后3小时和24小时处死成年小鼠，取出8个器官，胃，结肠，肝，肾，膀胱，肺，脑和骨髓。处理后3小时和24小时处死婴儿小鼠，切除肝脏。在另一项研究中，在成年小鼠的再生肝脏中研究了氟喹的遗传毒性。为此目的，用乙醚麻醉8周龄的雄性小鼠，取出肝脏，左侧外侧叶，左侧内侧叶和右侧外侧叶的3个主瓣。在肝切除术后4天，给小鼠口服氟喹一次。在FL处理后3小时处死它们并对再生的肝脏进行取样。用于彗星试验的载玻片在每个设定时间制备[1]。 |
| Kinase Experiment | 将含有0.4μg运动前体DNA和1U拓扑异构酶II的20μL反应混合物和每种抗菌剂(包括Flumequine)的连续稀释液在37℃下在含有20mM Tris-HCl(pH7.5)的缓冲液中温育5分钟，120mM KCl，10mM MgCl 2，1mM ATP，0.5mM二硫苏糖醇和30μg/ mL牛血清白蛋白。通过加入具有凝胶上样缓冲液的肌氨酸终止反应后，通过琼脂糖凝胶电泳分离链接和连接的kDNA。凝胶用溴化乙锭染色，并使用UV光(302nm)和凝胶印刷200i/VGA拍照，并用图像分析仪追踪条带的亮度。对每个条带进行定量，测量每种浓度的喹诺酮处理的DNA量，以确定对DNA促旋酶和拓扑异构酶II的50％抑制浓度[1]。 |
| Data Literature Source | [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. |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 50mg 100mg |
是一种喹诺酮类抗生素，为拓扑异构酶 II (Topoisomerase II) 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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