产品
编 号：F750914
分子式：C20H21F2N3O
分子量：357.4
分子式：C20H21F2N3O
分子量：357.4
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CAS No: 2290534-93-7
产品详情
生物活性：
MmpL3-IN-1 (compound 32) is a potent Mycobacterial membrane protein large 3 (MmpL3) inhibitor. MmpL3-IN-1 has anti-tuberculosis activity with the MIC<0.016 μg/mL in M. tuberculosis and can be used in studies of drug-resistant tuberculosis.
体内研究：
MmpL3-IN-1 (compound 32) (oral gavage, 100 mg/kg, 5 days per week, 30 days) has effective anti-tuberculosis activity in SPF BALB/c female mice with H37Rv.Animal Model:SPF BALB/c female mice with H37Rv
Dosage:100 mg/kg
Administration:Oral gavage; 5 days per week; 30 days
Result:Showed a 2.0 log CFU reduction of H37Rv in lung colony forming units.
Animal Model:BALB/c mouse (female) weighing 20-25 g
Dosage:
Administration:100 mg/kg p.o. or 10 mg/kg i.v. ; 0-24 hours
Result:b>The pharmacokinetic parameters of MmpL3-IN-1 (compound 32)Parameteriv, 10 mg/kgpo, 100 mg/kg
t1/2(h)7.377.48
Cmax (ng/mL)5105211
Tmax(h)0.030.5
AUC0-t(h?ng/mL)24751625
MRT0-t(h?ng/mL)2.008.69
V (mL/kg)42067-
CL (mL/h/kg)3958-
F%-6.6
体外研究：
MmpL3-IN-1 (compound 32) (0.26-64 μg/mL, 2-7days) has potent anti-M. tuberculosis activity with the MIC value of less than 0.016 μg/mL and with almost non-toxic to Vero cells.MmpL3-IN-1 has good microsomal stability and little inhibition of hERG K+ channels with the IC50 value of more than 30 μM.MmpL3-IN-1 (0.0625-1 μg/mL, 16 h) can inhibit TMM transport by targeting MmpL3, thereby affecting the formation of the cell wall of M. tuberculosis.
MmpL3-IN-1 (compound 32) is a potent Mycobacterial membrane protein large 3 (MmpL3) inhibitor. MmpL3-IN-1 has anti-tuberculosis activity with the MIC<0.016 μg/mL in M. tuberculosis and can be used in studies of drug-resistant tuberculosis.
体内研究：
MmpL3-IN-1 (compound 32) (oral gavage, 100 mg/kg, 5 days per week, 30 days) has effective anti-tuberculosis activity in SPF BALB/c female mice with H37Rv.Animal Model:SPF BALB/c female mice with H37Rv
Dosage:100 mg/kg
Administration:Oral gavage; 5 days per week; 30 days
Result:Showed a 2.0 log CFU reduction of H37Rv in lung colony forming units.
Animal Model:BALB/c mouse (female) weighing 20-25 g
Dosage:
Administration:100 mg/kg p.o. or 10 mg/kg i.v. ; 0-24 hours
Result:b>The pharmacokinetic parameters of MmpL3-IN-1 (compound 32)Parameteriv, 10 mg/kgpo, 100 mg/kg
t1/2(h)7.377.48
Cmax (ng/mL)5105211
Tmax(h)0.030.5
AUC0-t(h?ng/mL)24751625
MRT0-t(h?ng/mL)2.008.69
V (mL/kg)42067-
CL (mL/h/kg)3958-
F%-6.6
体外研究：
MmpL3-IN-1 (compound 32) (0.26-64 μg/mL, 2-7days) has potent anti-M. tuberculosis activity with the MIC value of less than 0.016 μg/mL and with almost non-toxic to Vero cells.MmpL3-IN-1 has good microsomal stability and little inhibition of hERG K+ channels with the IC50 value of more than 30 μM.MmpL3-IN-1 (0.0625-1 μg/mL, 16 h) can inhibit TMM transport by targeting MmpL3, thereby affecting the formation of the cell wall of M. tuberculosis.
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