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.
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Description | 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. |
Targets&IC50 | 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) |
In vitro | LeuRS-IN-1 (compound 13) hydrochloride exhibits potent antibacterial activity against M.tb H37Rv, showcasing a minimum inhibitory concentration (MIC) value of 0.02 μg/mL[1]. Additionally, LeuRS-IN-1 (compound 3a) hydrochloride demonstrates cytotoxic effects on HepG2 cells after 48 hours of exposure, with an effective concentration (EC 50) value of 65.8 μM[2]. |
In vivo | LeuRS-IN-1 hydrochloride, administered orally at a dosage of 100 mg/kg daily for 14 days, effectively reduces lung colony-forming unit (CFU) values in mice with acute tuberculosis (TB) [1]. A lower dosage of 33 mg/kg, administered orally five days a week for four weeks, significantly decreases lung and spleen CFU values in mice with chronic TB [1]. Pharmacokinetic studies in mice reveal that, following intravenous (i.v.) administration at 30 mg/kg, LeuRS-IN-1 exhibits a maximum concentration (C max) of 13.6 μg/ml at 5 minutes, a clearance (CL) of 582 ml/h/kg, a steady-state volume of distribution (V ss) of 3,142 ml/kg, a mean residence time (MRT) of 5.4 hours, an area under the curve (AUC) 0–∞ of 51.6 h · μg/ml, an alpha half-life (α-t 1/2) of 0.10 hours (2% AUC), and a beta half-life (β-t 1/2) of 3.83 hours (98% AUC). Oral administration (p.o.) at the same dose achieves a C max of 6.4 μg/ml at 0.25 hours, an AUC 0-24 of 47.5 h · μg/ml, a terminal half-life of 3.1 hours, and a bioavailability of 9.2%. In murine GKO (C57BL/6-Ifngtm1ts) model of acute TB, 100 mg/kg of LeuRS-IN-1, given orally daily for 14 days post-infection with M. tuberculosis Erdman, reduces lung CFU counts. Similarly, in the BALB/c model of chronic TB infection, 33 mg/kg administered orally five days a week for four weeks, starting 21 days post-low-dose aerosol infection with M. tuberculosis Erdman, leads to decreased lung and spleen CFU counts [1]. |
Molecular Weight | 277.94 |
Formula | C10H14BCl2NO3 |
CAS No. | 1364683-67-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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