| Bioactivity | LeuRS-IN-1 hydrochloride is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 hydrochloride has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively[1]. LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM)[2]. |
| Invitro | 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 EC50 value of 65.8 μM[2]. |
| In Vivo | 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 |
| Name | LeuRS-IN-1 hydrochloride |
| CAS | 1364683-67-9 |
| Formula | C10H14BCl2NO3 |
| Molar Mass | 277.94 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Palencia A, et al. Discovery of Novel Oral Protein Synthesis Inhibitors of Mycobacterium tuberculosis That Target Leucyl-tRNA Synthetase. Antimicrob Agents Chemother. 2016;60(10):6271-6280. Published 2016 Sep 23. [2]. Li X, et al. Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656). J Med Chem. 2017 Oct 12;60(19):8011-8026. |
LeuRS-IN-1 hydrochloride
CAS: 1364683-67-9 F: C10H14BCl2NO3 W: 277.94
LeuRS-IN-1 hydrochloride is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS
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