DX-619
DX-619 is an antibacterial agent. DX-619 inhibits bacterial type II topoisomerases, DNA gyrase (GyrA), and topoisomerase IV (GrlA). DX-619 can be used in research related to bacterial infections, pneumonia, and other conditions.
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- CAS No.: 431058-65-0
- Formule: C21H24FN3O4
- Masse moléculaire:401.43
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Stockage:
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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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
DX-619 (24 h) exhibits potent in vitro activity against Staphylococcus aureus and coagulase-negative staphylococci, with MIC50 values of 0.06 and 0.016 μg/mL, respectively[3].
DX-619 (24 h) inhibits Vancomycin (HY-B0671)-resistant Staphylococcus aureus strains (Hershey VRS2 and Michigan VRS1) with MIC values of 0.25 and 0.12 μg/mL, respectively[3].
DX-619 (24 h) exhibits bactericidal activity against all 13 of 13 staphylococcal strains (including VRSA) after 24 h at 4× MIC, and shows bactericidal activity against VRSA strains after 3 to 6 h at 2× MIC[3].
DX-619 exhibits activity against Imipenem (HY-B1369A)-resistant Bacteroides fragilis group strains, inhibiting 90.9% at ≤1 μg/mL, with an MIC90 of 1 μg/mL[5].
DX-619 exhibits activity against levofloxacin (HY-B0330)-resistant anaerobic Gram-positive cocci, with an MIC90 of 2 μg/mL and 100% susceptibility at ≤2 μg/mL[5].
DX-619 exhibits high activity against Clostridium species associated with gas gangrene, inhibiting all strains at MICs of ≤0.03 to 0.25 μg/mL[5].
DX-619 exhibits activity against Moxifloxacin (HY-66011A)-resistant Clostridium difficile strains, with MICs ranging from 0.5 to 2 μg/mL[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
DX-619 (10 mg/kg; i.p.; twice daily; 14 days) is highly effective against penicillin-resistant S. pneumoniae in a mouse pneumonia model, with an ED50 of 0.69 mg/kg/day, and reduces lung viable bacterial counts to 1.73 log10 CFU/mL[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CBA/J (female, 5-week-old, 16-20 g, intranasal inoculation of PSSP strain NU83127)[6]
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Dosage:Various doses (ED50 determination); 10 mg/kg (bacteriological study)
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Administration:i.p.; twice daily (ED50 determination); at 24, 36, and 48 h after inoculation (bacteriological study); 14 days
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Result:Achieved an ED50 of 9.15 mg/kg/day against PSSP pneumonia.
Reduced mean viable bacterial counts in lungs to 1.75 log10 CFU/mL.
Eradicated viable bacteria from four of seven murine lungs.
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Animal Model:CBA/J (female, 5-week-old, 16-20 g, intranasal inoculation of PRSP strain NU187)[6]
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Dosage:Various doses (ED50 determination); 10 mg/kg (bacteriological study)
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Administration:i.p.; twice daily (ED50 determination); at 24, 36, and 48 h after inoculation (bacteriological study); 14 days
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Result:Achieved an ED50 of 0.69 mg/kg/day against PRSP pneumonia.
Reduced mean viable bacterial counts in lungs to 1.73 log10 CFU/mL.
Eradicated viable bacteria from four of seven murine lungs.
Chemical Information
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CAS No. 431058-65-0
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Masse moléculaire 401.43
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Formule C21H24FN3O4
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SMILES
COC1=C2N([C@H]3[C@H](C3)F)C=C(C(C2=CC=C1N4C[C@H](C5(CC5)N)CC4)=O)C(O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[2]. Fujikawa K, et al. In vitro antibacterial activity of DX-619, a novel des-fluoro(6) quinolone. Antimicrobial agents and chemotherapy. 2005 Jul;49(7):3040-5. [Content Brief]
[3]. Bogdanovich T, et al. Antistaphylococcal activity of DX-619, a new des-F(6)-quinolone, compared to those of other agents. Antimicrobial agents and chemotherapy. 2005 Aug;49(8):3325-33. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DX-619 Related Classifications
HY-187934 Related Classifications
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