Product Introduction
Bioactivity


英文名: Flumequine

描述: Flumequine (R-802) 是一种喹诺酮类抗生素，对革兰氏阳性菌和革兰氏阴性菌均有效。它是拓扑异构酶 II 抑制剂， 抑制细胞分裂，IC50值为 15 μM (3.92 μg/mL)。

体外活性: 100 mg/L Flumequine在水草Lythrum salicariaL中,减少根、下胚轴和子叶的平均长度,并减少次生根的数量.口服10 mg/kg Flumequine给药后,总体清除率为0.024 L/h.kg(鳕鱼),0.14 L/h.kg(濑鱼),消除半衰期(t1/2 λ z)为75小时(鳕鱼),31小时(濑鱼).Flumequine口服给药后,生物利用度为65% (鳕鱼)和41% (濑鱼).口服4000 ppm Flumequine给药3小时,而不是24小时后,在成年小鼠的胃﹑结肠和膀胱中引起剂量依赖性DNA损伤.大西洋鲑鱼静脉注射给药Flumequine后,表观分布容积稳定在3.5l/kg,消除半衰期(t 1/2)为22.8小时,血浆药物浓度时间曲线下面积为140微克×小时/毫升.

体内活性: Flumequine在12种临床沙门氏菌分离株中的最小抑制浓度（MIC）为0.06 μg/mL到32 μg/mL。Flumequine对大多数耐药菌株的E（max）值高达16,这表明其对耐药表型的重要贡献。Flumequine累积试验证实,高E(max)值与较低水平的积累有关。Flumequine抑制真核生物的拓扑异构酶II,这是双链DNA断裂反应和细菌螺旋酶受到影响的原因,Flumequine对拓扑异构酶II的抑制作用与对细菌螺旋酶的影响高度相关。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 3 mg/mL (11.48 mM)


关键字: Flumequine | inhibit | Topoisomerase | Inhibitor | Bacterial | R802 | R 802 | Antibiotic

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相关库: ReFRAME Related Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compounds Library Max | Human Metabolite Library | Fluorochemical Library | Inhibitor Library | DNA Damage & Repair Compound Library | Anti-Bacterial Compound Library | Orally Active Compound Library | Bioactive Compound Library