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).
For research use only. We do not sell to patients.
- CAS No.: 2882904-64-3
- Formula: C21H16ClF2NO2
- Molecular Weight:387.81
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Target: Filamenting temperature-sensitive mutant Z (FtsZ)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | CC50 |
>20 μg/mL
Compound: 30
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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
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[PMID: 35763867] |
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.
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Cell Line:Vero cells (African green monkey kidney cells)
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Concentration:>20 μg/mL
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Incubation Time:72 hours
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Result:Exhibited the 50% cytotoxic concentration (CC50) >20 μg/mL, much more than the inhibition of B. subtilis ATCC9372 (MIC =0.016 μg/mL).
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Cell Line:S. aureus ATCC25923 and Bacillus ATCC9372
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Concentration:1×, 2×, 4×, 8× MIC; MIC =0.125 μg/mL (S. aureus); 0.016 μg/mL (Bacillus)
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Incubation Time:3, 6, 12, 24 hours
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Result:Reduced B. subtilis ATCC9372 and S. aureus ATCC25923 cells below the lowest detectable limit (103 CFU/ mL) in 3 h.
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.
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Animal Model:Male ICR mice (infected with S. aureus ATCC25923)[1]
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Dosage:25 mg/kg
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Administration:Intraperitoneal injection; 0.5 mL
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Result:Significantly reduced the bacteria burden and showed comparable in vivo efficacy with vancomycin.
Chemical Information
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CAS No. 2882904-64-3
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Molecular Weight 387.81
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Formula C21H16ClF2NO2
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SMILES
NC(C1=C(C=CC(OCC2=CC(C3=CC=C(C=C3C)Cl)=CC=C2)=C1F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FtsZ-IN-4 Related Classifications
HY-150754 Related Classifications
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