Powder: -20°C for 3 years | In solvent: -80°C for 1 year
FtsZ-IN-4, an orally active inhibitor of FtsZ (filamenting temperature-sensitive mutant Z), demonstrates remarkable antibacterial activity and favorable pharmaceutical properties. With low cytotoxicity (CC 50 <20 μg/mL) [1], FtsZ-IN-4 exhibits promising potential for therapeutic applications.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 10-14周 | ||
50 mg | ¥ 13,800 | 10-14周 | ||
100 mg | ¥ 17,500 | 10-14周 |
产品描述 | FtsZ-IN-4, an orally active inhibitor of FtsZ (filamenting temperature-sensitive mutant Z), demonstrates remarkable antibacterial activity and favorable pharmaceutical properties. With low cytotoxicity (CC 50 >20 μg/mL) [1], FtsZ-IN-4 exhibits promising potential for therapeutic applications. |
体外活性 | MIC: Minimum inhibition concentration; MBC: Minimum bactericidal concentration. FtsZ-IN-4 (compound 30) shows potent antibacterial activity to B. subtilis and S. aureus with MICs of 0.008-0.25 μg/mL, respectively [1]. FtsZ-IN-4 (0.064 μg/mL or 0.5 μg/mL; 0-24 h) shows rapid bactericidal properties within 3 h, and the MBC/MIC ratios are ≤4, satisfying CLSI standards [1]. FtsZ-IN-4 (>20 μg/mL; 72 h) exerts low cytotoxicity towards Vero cells [1]. FtsZ-IN-4 (0.016 μg/mL; 3 h) increases the length of the B. subtilis ATCC9372, causes abnormal bacterial cell division and lead to bacterial cell death [1]. FtsZ-IN-4 (10 μg/mL; 0-15 min) induces SaFtsZ polymerization and (0-35 μg/mL; 30 min) inhibits the GTPase activity of SaFtsZ in a dose-dependent manner [1]. Cell Cytotoxicity Assay [1] Cell Line: Vero cells (African green monkey kidney cells) Concentration: >20 μg/mL Incubation Time: 72 hours Result: Exhibited the 50% cytotoxic concentration (CC 50 ) >20 μg/mL, much more than the inhibition of B. subtilis ATCC9372 (MIC =0.016 μg/mL). Cell Proliferation Assay [1] Cell Line: S. aureus ATCC25923 and Bacillus ATCC9372 Concentration: 1×, 2×, 4×, 8× MIC; MIC =0.125 μg/mL ( S. aureus ); 0.016 μg/mL ( Bacillus ) Incubation Time: 3, 6, 12, 24 hours Result: Reduced B. subtilis ATCC9372 and S. aureus ATCC25923 cells below the lowest detectable limit (103 CFU/ mL) in 3 h. |
体内活性 | FtsZ-IN-4 (compound 30) (5 mg/kg; p.o.) exhibits moderate exposure (AUC (0-t) =544.2 h*ng/mL) and an oral bioavailability (F) of 61.2% in mice [1]. FtsZ-IN-4 (25 mg/kg; i.v.) exerts good in vivo efficacy in mice. Murine pharmacokinetic profiles of FtsZ-IN-4 [1] Route Dose (mg/kg) T 1/2 (h) T max (h) C max (ng/mL) AUC (0-t) (h ng/mL) AUC (0-∞) (h ng/mL) V ss (ng/mL) CL (mL/h/kg) F (%) i.v. 1 0.28 0.083 480.5 177.8 178.7 1545.5 5682.8 / 5 2.26 0.5 429.3 544.2 559.3 / / 61.2 Animal Model: Male ICR mice (infected with S. aureus ATCC25923) [1] Dosage: 25 mg/kg Administration: Intraperitoneal injection; 0.5 mL Result: Significantly reduced the bacteria burden and showed comparable in vivo efficacy with vancomycin. |
分子量 | 387.81 |
分子式 | C21H16ClF2NO2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
FtsZ-IN-4 Inhibitor inhibitor inhibit