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

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).

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FtsZ-IN-4

FtsZ-IN-4 Chemical Structure

CAS No. : 2882904-64-3

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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]

Cellular Effect
Cell Line Type Value Description References
Vero CC50
> 20 μg/mL
Compound: 30
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue staining based assay
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue staining based assay
[PMID: 35763867]
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].

MedChemExpress (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

MedChemExpress (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

CAS No.
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 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-150754
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