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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2882904-64-3
- 分子式: C21H16ClF2NO2
- 分子量:387.81
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
Target: Filamenting temperature-sensitive mutant Z (FtsZ)[1]
Cellular Effect
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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] |
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 2882904-64-3
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分子量 387.81
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
FtsZ-IN-4 関連分類
HY-150754 関連分類
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