2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial DNA/RNA Synthesis
  4. Antibacterial agent 338

Antibacterial agent 338 (Compound 65) is an antibacterial agent and GyrB inhibitor, with an IC50 of 12.60 nM against GyrB from E. coli. Antibacterial agent 338 binds to the ATP-binding domain of E. coli GyrB, thereby inhibiting the ATPase activity of GyrB. Antibacterial agent 338 exhibits broad-spectrum antibacterial activity against multidrug-resistant Gram-negative bacteria. Antibacterial agent 338 reduces bacterial load in a neutropenic mouse thigh infection model. Antibacterial agent 338 can be used for the research of Acinetobacter baumannii infection.

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Antibacterial agent 338

Antibacterial agent 338 Chemical Structure

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Antibacterial agent 338 Related Antibodies

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Description

Antibacterial agent 338 (Compound 65) is an antibacterial agent and GyrB inhibitor, with an IC50 of 12.60 nM against GyrB from E. coli. Antibacterial agent 338 binds to the ATP-binding domain of E. coli GyrB, thereby inhibiting the ATPase activity of GyrB. Antibacterial agent 338 exhibits broad-spectrum antibacterial activity against multidrug-resistant Gram-negative bacteria. Antibacterial agent 338 reduces bacterial load in a neutropenic mouse thigh infection model. Antibacterial agent 338 can be used for the research of Acinetobacter baumannii infection[1].

In Vitro

Antibacterial agent 338 (0.038-10000 nM; 60 min) potently inhibits the ATPase activity of E. coli DNA GyrB, with an IC50 value of 12.60 nM[1].
Antibacterial agent 338 (0.03-64 μg/mL; 18-20 h) exhibits broad-spectrum antibacterial activity against multidrug-resistant Gram-negative bacteria, with a MIC of 0.5 μg/mL against the multidrug-resistant *Acinetobacter baumannii* strain Aba-2024-D2-018[1].

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

Antibacterial agent 338 Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC0-t AUC0-∞ MRT0-∞ T1/2 CL_obs Vss_obs
Rat[1] 5 mg/kg i.v. 2057 ng/mL 961 ng·h/mL 971 ng·h/mL 2.12 h 2.66 h 87.2 mL/min/kg 11.1 L/kg
Mice[1] 20 mg/kg i.v. 35600 ng/mL 16164 16169 0.95 h 0.78 h 20.8 mL/min/kg 1.20 L/kg
In Vivo

Antibacterial agent 338 (10-20 mg/kg; intravenous injection; single dose, twice daily) exhibits dose-dependent in vivo efficacy against multidrug-resistant *Acinetobacter baumannii* in neutropenic mice[1].

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

Animal Model: ICR (half male and half female, 18-22 g, neutropenic via cyclophosphamide injection)[1]
Dosage: 10 mg/kg; 20 mg/kg; 20 mg/kg (two doses 6 hours apart)
Administration: i.v.; single dose; two doses 6 hours apart
Result: Achieved a bacterial burden reduction comparable to positive controls (levofloxacin and compound 9) at 20 mg/kg.
Produced a 2.65-log10 CFU/g reduction in bacterial burden.
Produced a 4.57-log10 CFU/g reduction, corresponding to >99.99% bacterial eradication, with bacterial burden reduced to pretreatment levels.
Molecular Weight

489.55

Formula

C25H28FN9O
SMILES

C/C([C@H](N)C)=C(C1)/CN1C2=NC(OC3=CN=C(NC4CC4)N=C3)=NC5=C2C6=CC(F)=CC(NC)=C6N5
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Room temperature in continental US; may vary elsewhere.
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References
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Antibacterial agent 338 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.

Keywords:

Antibacterial agent 338Antibacterial agent338Antibacterial agent-338BacterialDNA/RNA SynthesisE. coli GyrBGyrB ATPase activityneutropenic murine thigh infection modelhERG K+ channelCHO-hERG cellsAcinetobacter baumanniiDNA gyrase Bmultidrug-resistant acinetobacter baumannii infectionmultidrug-resistant Gram-negative bacteriaATP-binding domainInhibitorinhibitorinhibit

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