1. Anti-infection
  2. Bacterial
  3. FtsZ-IN-4

FtsZ-IN-4 

Cat. No.: HY-150754
Handling Instructions

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).

For research use only. We do not sell to patients.

FtsZ-IN-4 Chemical Structure

FtsZ-IN-4 Chemical Structure

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Description

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].

IC50 & Target

Target: Filamenting temperature-sensitive mutant Z (FtsZ)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 (CC50) >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.
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 Dose (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. 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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

387.81

Formula

C21H16ClF2NO2

SMILES

NC(C1=C(C=CC(OCC2=CC(C3=CC=C(C=C3C)Cl)=CC=C2)=C1F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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FtsZ-IN-4
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HY-150754
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