Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BTZ043 Racemate (Benzothiazinone 10526038) 是一种癸二烯基磷酰-β-D-核糖 2'-差向异构酶(DprE1) 抑制剂,用作新的抗分枝杆菌剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 315 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 970 | 现货 | ||
25 mg | ¥ 1,860 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,780 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 822 | 现货 |
产品描述 | BTZ043 Racemate (Benzothiazinone 10526038) is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor, used as a new antimycobacterial agent. |
体外活性 | By targeting decaprenylphosphoryl-β-D-ribose 2'-epimerase, BTZ043 abolishes the formation of decaprenylphosphoryl arabinose, leading to cell lysis and death of Mycobacterium tuberculosis. BTZ043 displays similar activity against all clinical isolates of M. tuberculosis, including multidrug-resistant and extensively drug-resistant strains. BTZ043 displays significant activity against M. tuberculosis H37Rv and Mycobacterium smegmatis with MIC of 1 ng/mL (2.3 nM) and 4 ng/mL (9.2 nM), respectively, which is more potent than those of the existing tuberculosis (TB) drugs isoniazid (INH) and ethambutol (EMB) with MIC of 0.02-0.2 μg/mL and 1-5 μg/mL, respectively. BTZ043 is less effective in two different model systems (auxotrophy and starvation) involving metabolically inert M. tuberculosis, indicating that BTZ043 blocks a step in active metabolism similar to isoniazid (INH). BTZ043 treatment in M. smegmatis cells decreases the growth rate rapidly followed by a swelling of the poles and lysis of the cells after a few hours, which is similar but delayed in M. tuberculosis. [1] BTZ043 (1/4 MIC 0.375 ng/mL) in combination with TMC207 (1/4 MIC 20 ng/mL) has a stronger cidal effect on M. tuberculosis but not BTZ-resistant M. tuberculosis mutant than TMC207 alone at a concentration of 80 ng/mL. [2] |
体内活性 | In a mouse model of chronic tuberculosis, administration of BTZ043 at 37.5 mg/kg or 300 mg/kg for 4 weeks reduces the bacterial burden in the lungs and spleens by 1 and 2 logs, respectively. [1] |
别名 | BTZ044, BTZ10526038, Benzothiazinone 10526038 |
分子量 | 431.39 |
分子式 | C17H16F3N3O5S |
CAS No. | 957217-65-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 21 mg/mL (48.7 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3181 mL | 11.5904 mL | 23.1809 mL | 57.9522 mL |
5 mM | 0.4636 mL | 2.3181 mL | 4.6362 mL | 11.5904 mL | |
10 mM | 0.2318 mL | 1.159 mL | 2.3181 mL | 5.7952 mL | |
20 mM | 0.1159 mL | 0.5795 mL | 1.159 mL | 2.8976 mL |
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。
BTZ043 Racemate 957217-65-1 Microbiology/Virology Others Antibacterial DprE1 Benzothiazinone10526038 inhibit Benzothiazinone-10526038 BTZ-044 BTZ044 Inhibitor BTZ-043 Racemate BTZ-043 BTZ-10526038 BTZ043 BTZ 043 tuberculosis BTZ10526038 Benzothiazinone 10526038 BTZ 10526038 BTZ 044 Bacterial inhibitor