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  3. LeuRS-IN-1 hydrochloride

LeuRS-IN-1 hydrochloride 

Cat. No.: HY-139987A
Handling Instructions

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. LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM).

For research use only. We do not sell to patients.

LeuRS-IN-1 hydrochloride Chemical Structure

LeuRS-IN-1 hydrochloride Chemical Structure

CAS No. : 1364683-67-9

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Description

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].

IC50 & Target[1][2]

M.tb LeuRS

0.06 μM (IC50)

M.tb LeuRS

0.075 μM (Kd)

human cytoplasmic LeuRS

38.8 μM (IC50)

HepG2 protein synthesis

19.6 μM (EC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 Dose (mg/kg) Cmax (μg/ml)
at 5 min
CL (ml/h/kg) Vss (ml/kg) MRT (h) AUC0-∞ 
(h · μg/ml)
α-t1/2 
(h) (% AUC)
β-t1/2 
(h) (% AUC)
i.v. 30 13.6 582 3,142 5.4 51.6 0.10 (2) 3.83 (98)
Administration Dose (mg/kg) Cmax (μg/ml) Tmax (h) AUC0-24 
(h · μg/ml)
Terminal 
t1/2 (h)
Bioavailability
(%) (h · μg/ml)
Mouse PPB
(%)
p.o. 30 6.4 0.25 47.5 3.1 9.2 23

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

277.94

Formula

C₁₀H₁₄BCl₂NO₃

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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LeuRS-IN-1 hydrochloride
Cat. No.:
HY-139987A
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