FtsZ-IN-4

Name: FtsZ-IN-4
Brand: TargetMol
SKU: T61737
Rating: 4.5 (1 reviews)

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产品编号 T61737

FtsZ-IN-4, an orally active inhibitor of FtsZ (filamenting temperature-sensitive mutant Z), demonstrates remarkable antibacterial activity and favorable pharmaceutical properties. With low cytotoxicity (CC 50 >20 μg/mL) [1], FtsZ-IN-4 exhibits promising potential for therapeutic applications.

FtsZ-IN-4

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产品编号 T61737

规格	价格	库存
25 mg	¥ 10,600	10-14周
50 mg	¥ 13,800	10-14周
100 mg	¥ 17,500	10-14周

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产品描述	FtsZ-IN-4, an orally active inhibitor of FtsZ (filamenting temperature-sensitive mutant Z), demonstrates remarkable antibacterial activity and favorable pharmaceutical properties. With low cytotoxicity (CC 50 >20 μg/mL) [1], FtsZ-IN-4 exhibits promising potential for therapeutic applications.
体外活性	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 [1]. 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 [1]. FtsZ-IN-4 (>20 μg/mL; 72 h) exerts low cytotoxicity towards Vero cells [1]. 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 [1]. 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 [1]. Cell Cytotoxicity Assay [1] Cell Line: Vero cells (African green monkey kidney cells) Concentration: >20 μg/mL Incubation Time: 72 hours Result: Exhibited the 50% cytotoxic concentration (CC 50 ) >20 μg/mL, much more than the inhibition of B. subtilis ATCC9372 (MIC =0.016 μg/mL). Cell Proliferation Assay [1] Cell Line: S. aureus ATCC25923 and Bacillus ATCC9372 Concentration: 1×, 2×, 4×, 8× MIC; MIC =0.125 μg/mL ( S. aureus ); 0.016 μg/mL ( Bacillus ) Incubation Time: 3, 6, 12, 24 hours Result: Reduced B. subtilis ATCC9372 and S. aureus ATCC25923 cells below the lowest detectable limit (103 CFU/ mL) in 3 h.
体内活性	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 [1]. FtsZ-IN-4 (25 mg/kg; i.v.) exerts good in vivo efficacy in mice. Murine pharmacokinetic profiles of FtsZ-IN-4 [1] Route Dose (mg/kg) T 1/2 (h) T max (h) C max (ng/mL) AUC (0-t) (h ng/mL) AUC (0-∞) (h ng/mL) V ss (ng/mL) CL (mL/h/kg) F (%) i.v. 1 0.28 0.083 480.5 177.8 178.7 1545.5 5682.8 / 5 2.26 0.5 429.3 544.2 559.3 / / 61.2 Animal Model: Male ICR mice (infected with S. aureus ATCC25923) [1] Dosage: 25 mg/kg Administration: Intraperitoneal injection; 0.5 mL Result: Significantly reduced the bacteria burden and showed comparable in vivo efficacy with vancomycin.