产品
编 号：F756576
分子式：C21H16ClF2NO2
分子量：387.81
分子式：C21H16ClF2NO2
分子量：387.81
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CAS No: 2882904-64-3
产品详情
生物活性：
FtsZ-IN-4 is an orally active FtsZ (filamenting temperature-sensitive mutant Z) inhibitor, exhibits excellent antibacterial activity. FtsZ-IN-4 shows good pharmaceutical properties with low cytotoxicity (CC50 >20 μg/mL).
体内研究：
FtsZ-IN-4 (compound 30) (5 mg/kg; p.o.) exhibits moderate exposure (AUC(0-t) =544.2 h*ng/mL) and an oral bioavailability (F) of 61.2% in mice.FtsZ-IN-4 (25 mg/kg; i.v.) exerts good in vivo efficacy in mice.Murine pharmacokinetic profiles of FtsZ-IN-4RouteDose (mg/kg)T1/2 (h)Tmax (h)Cmax (ng/mL)AUC(0-t) (h?ng/mL)AUC(0-∞) (h?ng/mL)Vss (ng/mL)CL (mL/h/kg)F (%)
i.v.10.280.083480.5177.8178.71545.55682.8/
52.260.5429.3544.2559.3//61.2
Animal Model:Male ICR mice (infected with S. aureus ATCC25923)
Dosage:25 mg/kg
Administration:Intraperitoneal injection; 0.5 mL
Result:Significantly reduced the bacteria burden and showed comparable in vivo efficacy with vancomycin.
体外研究：
MIC: Minimum inhibition concentration; MBC: Minimum bactericidal concentration.FtsZ-IN-4 (compound 30) shows potent antibacterial activity to B. subtilis and S. aureus with MICs of 0.008-0.25 μg/mL, respectively.FtsZ-IN-4 (0.064 μg/mL or 0.5 μg/mL; 0-24 h) shows rapid bactericidal properties within 3 h, and the MBC/MIC ratios are ≤4, satisfying CLSI standards.FtsZ-IN-4 (>20 μg/mL; 72 h) exerts low cytotoxicity towards Vero cells .FtsZ-IN-4 (0.016 μg/mL; 3 h) increases the length of the B. subtilis ATCC9372, causes abnormal bacterial cell division and lead to bacterial cell death.FtsZ-IN-4 (10 μg/mL; 0-15 min) induces SaFtsZ polymerization and (0-35 μg/mL; 30 min) inhibits the GTPase activity of SaFtsZ in a dose-dependent manner.
FtsZ-IN-4 is an orally active FtsZ (filamenting temperature-sensitive mutant Z) inhibitor, exhibits excellent antibacterial activity. FtsZ-IN-4 shows good pharmaceutical properties with low cytotoxicity (CC50 >20 μg/mL).
体内研究：
FtsZ-IN-4 (compound 30) (5 mg/kg; p.o.) exhibits moderate exposure (AUC(0-t) =544.2 h*ng/mL) and an oral bioavailability (F) of 61.2% in mice.FtsZ-IN-4 (25 mg/kg; i.v.) exerts good in vivo efficacy in mice.Murine pharmacokinetic profiles of FtsZ-IN-4RouteDose (mg/kg)T1/2 (h)Tmax (h)Cmax (ng/mL)AUC(0-t) (h?ng/mL)AUC(0-∞) (h?ng/mL)Vss (ng/mL)CL (mL/h/kg)F (%)
i.v.10.280.083480.5177.8178.71545.55682.8/
52.260.5429.3544.2559.3//61.2
Animal Model:Male ICR mice (infected with S. aureus ATCC25923)
Dosage:25 mg/kg
Administration:Intraperitoneal injection; 0.5 mL
Result:Significantly reduced the bacteria burden and showed comparable in vivo efficacy with vancomycin.
体外研究：
MIC: Minimum inhibition concentration; MBC: Minimum bactericidal concentration.FtsZ-IN-4 (compound 30) shows potent antibacterial activity to B. subtilis and S. aureus with MICs of 0.008-0.25 μg/mL, respectively.FtsZ-IN-4 (0.064 μg/mL or 0.5 μg/mL; 0-24 h) shows rapid bactericidal properties within 3 h, and the MBC/MIC ratios are ≤4, satisfying CLSI standards.FtsZ-IN-4 (>20 μg/mL; 72 h) exerts low cytotoxicity towards Vero cells .FtsZ-IN-4 (0.016 μg/mL; 3 h) increases the length of the B. subtilis ATCC9372, causes abnormal bacterial cell division and lead to bacterial cell death.FtsZ-IN-4 (10 μg/mL; 0-15 min) induces SaFtsZ polymerization and (0-35 μg/mL; 30 min) inhibits the GTPase activity of SaFtsZ in a dose-dependent manner.
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