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.
For research use only. We do not sell to patients.
- CAS No.: 431058-65-0
- Formula: C21H24FN3O4
- Molecular Weight:401.43
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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
Description
In Vitro
DX-619 (12.5-200 μM; 5-30 min) is a mechanism-based inhibitor of CYP3A4 in human liver microsomes, with a KI of 67.9 μM and a kinact of 0.0730 min-1[1].
DX-619 inhibits OAT3-mediated 6β-OHF uptake with a Ki of 239 μM[1].
DX-619 inhibits MATE1-mediated 6β-OHF uptake with a Ki of 4.32 μM[1].
DX-619 (20-48 h) exhibits the most potent antibacterial activity against Gram-positive bacteria among the tested compounds, including Ciprofloxacin (HY-B0356)-resistant MRSA (MIC90 0.5 μg/mL), MRCNS, VRE, and Ciprofloxacin (HY-B0356)-resistant S. pneumoniae[2].
DX-619 (20 h) exhibits good antibacterial activity against Gram-negative bacteria, including Haemophilus influenzae, Moraxella catarrhalis, Enterobacteriaceae, and Acinetobacter species[2].
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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Molecular Weight 401.43
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Formula 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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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)
DX-619 Related Classifications
HY-187934 Related Classifications
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