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  4. LeuRS-IN-1 hydrochloride

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).

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LeuRS-IN-1 hydrochloride Chemical Structure

LeuRS-IN-1 hydrochloride Chemical Structure

CAS No. : 1364683-67-9

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LeuRS-IN-1 hydrochloride Related Antibodies

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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)

Cellular Effect
Cell Line Type Value Description References
HepG2 EC50
65.8 μM
Compound: 3a
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay
[PMID: 28953378]
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].

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

LeuRS-IN-1 hydrochloride Related Antibodies
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

MedChemExpress (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.
SMILES

CCOC1=C2C([C@H](OB2O)CN)=C(C=C1)Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LeuRS-IN-1 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LeuRS-IN-11364683-67-9BacterialtuberculosisM. tuberculosisHepG2protein synthesishuman cytoplasmiccellsmiceInhibitorinhibitorinhibit

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