| Bioactivity | 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)[1]. |
| Target | Target: Filamenting temperature-sensitive mutant Z (FtsZ) |
| Invitro | 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: |
| In Vivo | 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 |
| Name | FtsZ-IN-4 |
| Formula | C21H16ClF2NO2 |
| Molar Mass | 387.81 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Deng J, et al. Design, synthesis and biological evaluation of biphenyl-benzamides as potent FtsZ inhibitors. Eur J Med Chem. 2022 Sep 5. 239:114553. |