DK 507k
DK 507k is an orally active 8-methoxyquinolone Antibacterial agent. DK 507k targets DNA gyrase subunit A (GyrA) and modulates the function of GyrA. DK 507k inhibits the growth of various Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa and Methicillin (HY-121544)-resistant Staphylococcus aureus. DK 507k eliminates Penicillin-tolerant Streptococcus pneumoniae from the lungs of mice. DK 507k can be used in research related to sepsis and *Streptococcus pneumoniae* pneumonia.
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- No. CAS: 364069-14-7
- Fòrmula: C20H21F2N3O4
- Peso molecular:405.40
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Almacenamiento:
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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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
DNA Gyrase |
In Vitro
DK 507k (18 h) exhibits potent in vitro activity against a broad range of gram-positive bacterial clinical isolates, including quinolone-resistant strains, with MIC90 values ranging from 0.06 μg/mL (ofloxacin-susceptible methicillin-resistant S. aureus) to 8 μg/mL (E. faecium)[1].
DK 507k (18 h; 96 h for Legionella pneumophila; 14 days for Mycoplasma pneumoniae) exhibits potent in vitro activity against a broad range of gram-negative bacterial clinical isolates, with MIC90 values ranging from 0.008 μg/mL (H. influenzae) to 1 μg/mL (K. pneumoniae, S. marcescens, Enterobacter spp., indole-positive Proteus, ofloxacin-susceptible P. aeruginosa, ofloxacin-resistant N. gonorrhoeae)[1].
DK 507k (4 μg/mL) has low protein binding (26.7%) to mouse serum in vitro[1].
DK 507k potently inhibits quinolone-susceptible Streptococcus pneumoniae (penicillin-susceptible, -intermediate, and -resistant strains) with an MIC50 of 0.06 μg/mL and an MIC90 of 0.125 μg/mL[2].
DK 507k potently inhibits quinolone-resistant Streptococcus pneumoniae strains with an MIC50 of 0.25 μg/mL and an MIC90 of 0.5 μg/mL, and it is not a substrate for efflux mechanisms in these strains[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
DK 507k (7.5-30 mg/kg/day; s.c.; twice daily; 3 days) demonstrates dose-dependent, potent efficacy against penicillin-resistant S. pneumoniae pneumonia in mice, with complete bacterial clearance from lungs observed at 30 mg/kg/day, unlike comparator fluoroquinolones[1].
DK 507k (10-20 mg/kg/day; p.o.; once daily; 3 days) exhibits potent efficacy against foreign body-associated urinary tract infection caused by P. aeruginosa in rats, with significant reductions in bacterial burden across all tested tissues and superior activity to ciprofloxacin at equivalent doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Slc:ddy (5-week-old male, intraperitoneal bacterial challenge)[1]
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Dosage:1.07 mg/kg (MSSA); 9.23 mg/kg (MRSA); 3.63 mg/kg (PSSP); 1.49 mg/kg (PRSP); 4.19 mg/kg (E. coli); 3.23 mg/kg (P. aeruginosa)
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Administration:i.v.; single dose immediately post-infection
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Result:Exhibited an ED50 of 1.07 mg/kg against MSSA 037114.
Exhibited an ED50 of 9.23 mg/kg against MRSA 037004.
Exhibited an ED50 of 3.63 mg/kg against PSSP 037288.
Exhibited an ED50 of 1.49 mg/kg against PRSP 033890.
Exhibited an ED50 of 4.19 mg/kg against E. coli 037042.
Exhibited an ED50 of 3.23 mg/kg against P. aeruginosa 037096.
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Animal Model:CBA/JNCrj (4-week-old male, intranasal penicillin-resistant S. pneumoniae inoculation)[1]
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Dosage:7.5 mg/kg/day; 15 mg/kg/day; 30 mg/kg/day
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Administration:s.c.; twice daily; 3 days
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Result:Reduced lung bacterial counts in a dose-dependent manner.
At 15 mg/kg/day, lowered lung bacterial counts significantly compared to untreated controls, moxifloxacin-treated groups, and gatifloxacin-treated groups.
At 30 mg/kg/day, eliminated bacteria from the lungs to levels near the detection limit (≤2.30 log10 CFU/g lung tissue), while gatifloxacin and moxifloxacin showed no significant efficacy.
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Animal Model:Crj:CD(S-D)IGS (7-week-old female, transurethral polyethylene tube placement followed by P. aeruginosa inoculation)[1]
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Dosage:10 mg/kg/day; 20 mg/kg/day
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Administration:p.o.; once daily; 3 days
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Result:Significantly reduced bacterial counts in kidneys, bladder, and polyethylene tubes compared to untreated controls.
At 20 mg/kg/day, reduced bacterial counts on the polyethylene tube by approximately 4.5 log10 CFU/PT (from 7.50 to 3.00 log10 CFU/PT) and showed greater efficacy than ciprofloxacin against bladder and tube-associated bacteria.
Chemical Information
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No. CAS 364069-14-7
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Peso molecular 405.40
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Fòrmula C20H21F2N3O4
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SMILES
N[C@H]1C2(CN(C1)C=3C(OC)=C4N(C=C(C(O)=O)C(=O)C4=CC3F)[C@H]5[C@@H](F)C5)CC2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1].
Otani T, et al. In vitro and in vivo antibacterial activities of DK-507k, a novel fluoroquinolone. Antimicrob Agents Chemother. 2003 Dec;47(12):3750-9.
[Content Brief]
[2]. Browne FA, et al. Antipneumococcal activity of DK-507k, a new quinolone, compared with the activities of 10 other agents. Antimicrob Agents Chemother. 2003 Dec;47(12):3815-24. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DK 507k Related Classifications
HY-107044 Related Classifications
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