LeuRS-IN-1
LeuRS-IN-1 is a potent, orally active M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS) inhibitor. LeuRS-IN-1 has IC50 and Kd values of 0.06 μM, 0.075 μM for M.tb LeuRS, respectively. LeuRS-IN-1 inhibits human cytoplasmic LeuRS (IC50=38.8 μM), and HepG2 protein synthesis (EC50=19.6 μM).
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- CAS. Nr.: 1364914-72-6
- Formel: C10H13BClNO3
- Molecular Weight:241.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
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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
In Vivo
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) | 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.
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Animal Model:Murine GKO (C57BL/6-Ifngtm1ts) model of acute TB[1]
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Dosage:100 mg/kg
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Administration:Orally daily for 14 days after 10 days of infection (start) with M. tuberculosis Erdman.
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Result:Reduced lung CFU value in mice.
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Animal Model:Murine BALB/c model of chronic TB infection[1]
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Dosage:33 mg/kg
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Administration:Orally 5 days a week for 4 weeks after infection with M. tuberculosis Erdman with a low-dose aerosol 21 days prior (start).
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Result:Reduced lung and spleen CFU values in mice.
Chemical Information
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CAS. Nr. 1364914-72-6
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Molecular Weight 241.48
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Formel C10H13BClNO3
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SMILES
CCOC1=C2C([C@H](OB2O)CN)=C(C=C1)Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
LeuRS-IN-1 Related Classifications
HY-139987 Related Classifications
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