Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LeuRS-IN-1 hydrochloride is a potent and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS). It has IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively, for M.tb LeuRS. Additionally, LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS with an IC 50 of 38.8 μM and HepG2 protein synthesis with an EC 50 of 19.6 μM.
产品描述 | LeuRS-IN-1 hydrochloride is a potent and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS). It has IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively, for M.tb LeuRS. Additionally, LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS with an IC 50 of 38.8 μM and HepG2 protein synthesis with an EC 50 of 19.6 μM. |
靶点活性 | LeuRS (M. tuberculosis):0.06 μM (IC50), LeuRS (M. tuberculosis):0.075 μM (Kd), Protein synthesis (HepG2 cells):19.6 μM (EC50), LeuRS (Human cytoplasmic):38.8 μM (IC50) |
体外活性 | LeuRS-IN-1 (compound 13) hydrochloride has a MIC value of 0.02 μg/mL for M.tb H37Rv bacteria[1]. LeuRS-IN-1 (compound 3a) (48 h) hydrochloride induces HepG2 cell toxicity with an EC 50 value of 65.8 μM[2]. |
体内活性 | LeuRS-IN-1 (100 mg/kg; orally daily for 14 days) hydrochloride reduces lung CFU value in acute tuberculosis (TB) mice[1]. LeuRS-IN-1 (33 mg/kg; orally 5 days a week for 4 weeks) hydrochloride reduces lung and spleen CFU values in chronic TB mice[1]. Murine pharmacokinetic parameters[1]: Administration Dose (mg/kg) C max (μg/ml) at 5 min CL (ml/h/kg) V ss (ml/kg) MRT (h) AUC 0-∞ (h · μg/ml) α-t 1/2 (h) (% AUC) β-t 1/2 (h) (% AUC) i.v. 30 13.6 582 3,142 5.4 51.6 0.10 (2) 3.83 (98) Administration Dose (mg/kg) C max (μg/ml) T max (h) AUC 0-24 (h · μg/ml) Terminal t 1/2 (h) Bioavailability (%) (h · μg/ml) Mouse PPB (%) p.o. 30 6.4 0.25 47.5 3.1 9.2 23 Animal Model: Murine GKO (C57BL/6-Ifngtm1ts) model of acute TB[1]Dosage: 100 mg/kg Administration: Orally daily for 14 days after 10 days of infection (start) with M. tuberculosis Erdman. Result: Reduced lung CFU value in mice. Animal Model: Murine BALB/c model of chronic TB infection[1]Dosage: 33 mg/kg Administration: Orally 5 days a week for 4 weeks after infection with M. tuberculosis Erdman with a low-dose aerosol 21 days prior (start). Result: Reduced lung and spleen CFU values in mice. |
分子量 | 277.94 |
分子式 | C10H14BCl2NO3 |
CAS No. | 1364683-67-9 |
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。
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