产品
编 号：F744424
分子式：C10H13BClNO3
分子量：241.48
分子式：C10H13BClNO3
分子量：241.48
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CAS No: 1364914-72-6
产品详情
生物活性：
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).
体内研究：
LeuRS-IN-1 (100 mg/kg; orally daily for 14 days) reduces lung CFU value in acute tuberculosis (TB) mice.LeuRS-IN-1 (33 mg/kg; orally 5 days a week for 4 weeks) reduces lung and spleen CFU values in chronic TB mice.Murine pharmacokinetic parameters:AdministrationDose (mg/kg)Cmax (μg/ml)at 5 minCL (ml/h/kg)Vss?(ml/kg)MRT (h)AUC0-∞?(h · μg/ml)α-t1/2?(h) (% AUC)β-t1/2?(h) (% AUC)
i.v.3013.65823,1425.451.60.10 (2)3.83 (98)
AdministrationDose (mg/kg)Cmax?(μg/ml)Tmax?(h)AUC0-24?(h · μg/ml)Terminal?t1/2?(h)Bioavailability (%)?(h · μg/ml)Mouse PPB (%)
p.o.306.40.2547.53.19.223
Animal Model:Murine GKO (C57BL/6-Ifngtm1ts) model of acute TB
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
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.
体外研究：
LeuRS-IN-1 (compound 13) has a MIC value of 0.02 μg/mL for M.tb H37Rv bacteria.LeuRS-IN-1 (compound 3a) (48 h) induces HepG2 cell toxicity with an EC50 value of 65.8 μM.
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).
体内研究：
LeuRS-IN-1 (100 mg/kg; orally daily for 14 days) reduces lung CFU value in acute tuberculosis (TB) mice.LeuRS-IN-1 (33 mg/kg; orally 5 days a week for 4 weeks) reduces lung and spleen CFU values in chronic TB mice.Murine pharmacokinetic parameters:AdministrationDose (mg/kg)Cmax (μg/ml)at 5 minCL (ml/h/kg)Vss?(ml/kg)MRT (h)AUC0-∞?(h · μg/ml)α-t1/2?(h) (% AUC)β-t1/2?(h) (% AUC)
i.v.3013.65823,1425.451.60.10 (2)3.83 (98)
AdministrationDose (mg/kg)Cmax?(μg/ml)Tmax?(h)AUC0-24?(h · μg/ml)Terminal?t1/2?(h)Bioavailability (%)?(h · μg/ml)Mouse PPB (%)
p.o.306.40.2547.53.19.223
Animal Model:Murine GKO (C57BL/6-Ifngtm1ts) model of acute TB
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
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.
体外研究：
LeuRS-IN-1 (compound 13) has a MIC value of 0.02 μg/mL for M.tb H37Rv bacteria.LeuRS-IN-1 (compound 3a) (48 h) induces HepG2 cell toxicity with an EC50 value of 65.8 μM.
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