产品
编 号：F752588
分子式：C20H21N3O5S
分子量：415.46
分子式：C20H21N3O5S
分子量：415.46
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CAS No: 2419160-96-4
产品详情
生物活性：
DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis.
体内研究：
DprE1-IN-4 exhibits acceptable pharmacokinetic property after p.o. and i.v., DprE1-IN-4 (oral administration, 50 mg/kg) exhibits high plasma exposure ((AUC)0-∞=657 ng·h/mL) and high maximum plasma concentration (Cmax=486 ng/mL). It exhibits oral bioavailability (F=7.9%) and is deemed worthy of further evaluation in?in vivo?efficacy studies.DprE1-IN-4 (oral gavage; 100 mg/kg; once daily; 3 weeks) showed potent?in vivo?activity, reducing the bacterial burden in the lungs by 2.02?log10?CFU compared with the untreated control group.
体外研究：
DprE1-IN-4 displays potent activity against?M. tuberculosis, it is against isolated clinical strains H37Rv, 13946a, 14862b and PBTZ169-resistant strain with MIC values of 0.12 μg/mL, 0.24 μg/mL, 0.24 μg/mL and 0.48 μg/mL, respectively.DprE1-IN-4 (0.76-16 μg/mL) shows a decrease in potency against only DprE1-overexpressing strains but not against DprE2-overexpressing and wild-type strains.?The IC50 value is 0.9±0.2 μg/mL for ?DprE1.
DprE1-IN-4 is a potent and orally active noncovalent DprE1 inhibitor with an IC50 of 0.90 μg/mL. DprE1-IN-4 exhibits potent in vitro activity against M. tuberculosis H37Rv and drug-resistant tuberculosis strain with MIC values of 0.12 μg/mL and 0.24 μg/mL, respectively. DprE1-IN-4 displays acceptable pharmacokinetic property and shows significant bactericidal activity in an acute mouse model of tuberculosis.
体内研究：
DprE1-IN-4 exhibits acceptable pharmacokinetic property after p.o. and i.v., DprE1-IN-4 (oral administration, 50 mg/kg) exhibits high plasma exposure ((AUC)0-∞=657 ng·h/mL) and high maximum plasma concentration (Cmax=486 ng/mL). It exhibits oral bioavailability (F=7.9%) and is deemed worthy of further evaluation in?in vivo?efficacy studies.DprE1-IN-4 (oral gavage; 100 mg/kg; once daily; 3 weeks) showed potent?in vivo?activity, reducing the bacterial burden in the lungs by 2.02?log10?CFU compared with the untreated control group.
体外研究：
DprE1-IN-4 displays potent activity against?M. tuberculosis, it is against isolated clinical strains H37Rv, 13946a, 14862b and PBTZ169-resistant strain with MIC values of 0.12 μg/mL, 0.24 μg/mL, 0.24 μg/mL and 0.48 μg/mL, respectively.DprE1-IN-4 (0.76-16 μg/mL) shows a decrease in potency against only DprE1-overexpressing strains but not against DprE2-overexpressing and wild-type strains.?The IC50 value is 0.9±0.2 μg/mL for ?DprE1.
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