Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MmpL3-IN-1, also known as compound 32, is a highly effective inhibitor of Mycobacterial membrane protein large 3 (MmpL3). With an anti-tuberculosis activity exhibiting a minimum inhibitory concentration (MIC) of less than 0.016 μg/mL in M. tuberculosis, MmpL3-IN-1 is a valuable compound for research on drug-resistant tuberculosis [1].
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | MmpL3-IN-1, also known as compound 32, is a highly effective inhibitor of Mycobacterial membrane protein large 3 (MmpL3). With an anti-tuberculosis activity exhibiting a minimum inhibitory concentration (MIC) of less than 0.016 μg/mL in M. tuberculosis, MmpL3-IN-1 is a valuable compound for research on drug-resistant tuberculosis [1]. |
体外活性 | MmpL3-IN-1 (compound 32) (0.26-64 μg/mL, 2-7days) has potent anti- M. tuberculosis activity with the MIC value of less than 0.016 μg/mL and with almost non-toxic to Vero cells [1]. MmpL3-IN-1 has good microsomal stability and little inhibition of hERG K + channels with the IC 50 value of more than 30 μM [1]. MmpL3-IN-1 (0.0625-1 μg/mL, 16 h) can inhibit TMM transport by targeting MmpL3, thereby affecting the formation of the cell wall of M. tuberculosis [1]. Cell Viability Assay [1] Cell Line: Vero cells Concentration: 0.26-64 μg/mL Incubation Time: 48 hours Result: Inhibited cell viability with an IC 50 value of 35.3 μg/mL. Western Blot Analysis [1] Cell Line: M. tuberculosis H37Rv mc 2 6206 Concentration: 0.0625-1 μg/mL Incubation Time: 16 hours Result: Resulted in the accumulation of alginate monomycin (TMM) expression and reduced cell wall-bound mycolic acid methyl esters (MAMEs) in a dose-dependent manner. Reduced synthesis of alginate dimycolate (TDM), together with accumulation of free mycolate at high concentration. |
体内活性 | MmpL3-IN-1 (compound 32) (oral gavage, 100 mg/kg, 5 days per week, 30 days) has effective anti-tuberculosis activity in SPF BALB/c female mice with H37Rv [1]. Animal Model: SPF BALB/c female mice with H37Rv [1] Dosage: 100 mg/kg Administration: Oral gavage; 5 days per week; 30 days Result: Showed a 2.0 log CFU reduction of H37Rv in lung colony forming units. Animal Model: BALB/c mouse (female) weighing 20-25 g [1] Dosage: Administration: 100 mg/kg p.o. or 10 mg/kg i.v.; 0-24 hours Result: b>The pharmacokinetic parameters of MmpL3-IN-1 (compound 32) Parameter iv, 10 mg/kg po, 100 mg/kg t 1/2 (h) 7.37 7.48 C max (ng/mL) 5105 211 T max (h) 0.03 0.5 AUC 0-t (h ng/mL) 2475 1625 MRT 0-t (h ng/mL) 2.00 8.69 V (mL/kg) 42067 - CL (mL/h/kg) 3958 - F% - 6.6 |
分子量 | 357.4 |
分子式 | C20H21F2N3O |
CAS No. | 2290534-93-7 |
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。
MmpL3-IN-1 2290534-93-7 Inhibitor inhibitor inhibit