Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LeuRS-IN-1 is a highly potent and orally active inhibitor of the leucyl-tRNA synthetase enzyme derived from Mycobacterium tuberculosis (M.tb LeuRS). It exhibits significant inhibitory activity against M.tb LeuRS with IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively. Additionally, LeuRS-IN-1 effectively inhibits human cytoplasmic LeuRS with an IC 50 value of 38.8 μM and suppresses protein synthesis in HepG2 cells with an EC 50 value of 19.6 μM.
产品描述 | LeuRS-IN-1 is a highly potent and orally active inhibitor of the leucyl-tRNA synthetase enzyme derived from Mycobacterium tuberculosis (M.tb LeuRS). It exhibits significant inhibitory activity against M.tb LeuRS with IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively. Additionally, LeuRS-IN-1 effectively inhibits human cytoplasmic LeuRS with an IC 50 value of 38.8 μM and suppresses protein synthesis in HepG2 cells with an EC 50 value 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) has a MIC value of 0.02 μg/mL for M.tb H37Rv bacteria[1]. LeuRS-IN-1 (compound 3a) (48 h) 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) reduces lung CFU value in acute tuberculosis (TB) mice[1]. LeuRS-IN-1 (33 mg/kg; orally 5 days a week for 4 weeks) 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 | 241.48 |
分子式 | C10H13BClNO3 |
CAS No. | 1364914-72-6 |
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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