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编 号：F755737
分子式：C20H24F2N4O5S2
分子量：502.56
分子式：C20H24F2N4O5S2
分子量：502.56
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CAS No: 2764818-29-1
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生物活性：
Antitubercular agent-31 (Compound 2) is an antitubercular agent with an MIC of 0.03 μM against M. tuberculosis H37Rv. Antitubercular agent-31 also inhibits DprE1 with an IC50 of 1.1 μM.
体内研究：
Antitubercular agent-31 (10 or 2 mg/kg; p.o. or i.v.; once) displays an acceptable pharmacokinetics (PK) profile with only dosing i.v., shows either poor membrane permeability or rapid clearance rate in vivo.Animal Model:Male Balb/c mice
Dosage:10 mg/kg or 2 mg/kg
Administration:Oral (10 mg/kg) or intravenous (2 mg/kg) administration (Pharmacokinetic Analysis)
Result:PK data for Antitubercular agent-31 (Compound 2),iv, 2mg/kg.Tmax (h)Cmax (ng/mL) AUC0-t(h*ng/mL) AUC0-∞(h*ng/mL) T1/2 (h) CL/F(mL/h/kg) MRT0-∞(h)
0.1±0.0463.4±103.4158.2±18.8161.3±18.60.3±0.012515.5±1379.70.4±0.0
No compound signal was detected at oral administration.
体外研究：
Antitubercular agent-31 (Compound 2) shows aqueous solubility of 0.81 μg/mL in phosphate buffer pH 7.4. The plasma protein binding property is 97.9%.Antitubercular agent-31 shows acceptable liver microsomal stability in human and mouse liver microsomes.
Antitubercular agent-31 (Compound 2) is an antitubercular agent with an MIC of 0.03 μM against M. tuberculosis H37Rv. Antitubercular agent-31 also inhibits DprE1 with an IC50 of 1.1 μM.
体内研究：
Antitubercular agent-31 (10 or 2 mg/kg; p.o. or i.v.; once) displays an acceptable pharmacokinetics (PK) profile with only dosing i.v., shows either poor membrane permeability or rapid clearance rate in vivo.Animal Model:Male Balb/c mice
Dosage:10 mg/kg or 2 mg/kg
Administration:Oral (10 mg/kg) or intravenous (2 mg/kg) administration (Pharmacokinetic Analysis)
Result:PK data for Antitubercular agent-31 (Compound 2),iv, 2mg/kg.Tmax (h)Cmax (ng/mL) AUC0-t(h*ng/mL) AUC0-∞(h*ng/mL) T1/2 (h) CL/F(mL/h/kg) MRT0-∞(h)
0.1±0.0463.4±103.4158.2±18.8161.3±18.60.3±0.012515.5±1379.70.4±0.0
No compound signal was detected at oral administration.
体外研究：
Antitubercular agent-31 (Compound 2) shows aqueous solubility of 0.81 μg/mL in phosphate buffer pH 7.4. The plasma protein binding property is 97.9%.Antitubercular agent-31 shows acceptable liver microsomal stability in human and mouse liver microsomes.
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