2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial Topoisomerase
  4. 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.

For research use only. We do not sell to patients.

DK 507k

DK 507k Chemical Structure

CAS No. : 364069-14-7

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DK 507k Related Antibodies

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Topoisomerase Topo I Topo II DNA gyrase

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Description

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[1][2].

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.

DK 507k Related Antibodies
Parmacokinetics
Species Dose Route AUC T1/2
Mice[1] 10 mg/kg i.v. 2.93 μg·h/mL 0.83 h
Mice[1] 15 mg/kg s.c. 3.60 (from 0 to 6 h) (sera) μg·h/mL /
Rat[1] 20 mg/kg p.o. 1.91 (from 0 to 6 h) (sera) μg·h/mL /
In Vivo

DK 507k (1.07-9.23 mg/kg; i.v.; single dose immediately post-infection) exhibits potent efficacy against systemic septicemia in mice, with ED50 values ranging from 1.07 to 9.23 mg/kg depending on the infecting pathogen, and is more effective than comparator fluoroquinolones against gram-positive organisms[1].
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.

Animal Model: Slc:ddy (5-week-old male, intraperitoneal bacterial challenge)[1]
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)
Administration: i.v.; single dose immediately post-infection
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.
Animal Model: CBA/JNCrj (4-week-old male, intranasal penicillin-resistant S. pneumoniae inoculation)[1]
Dosage: 7.5 mg/kg/day; 15 mg/kg/day; 30 mg/kg/day
Administration: s.c.; twice daily; 3 days
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.
Animal Model: Crj:CD(S-D)IGS (7-week-old female, transurethral polyethylene tube placement followed by P. aeruginosa inoculation)[1]
Dosage: 10 mg/kg/day; 20 mg/kg/day
Administration: p.o.; once daily; 3 days
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.
Molecular Weight

405.40

Formula

C20H21F2N3O4
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DK 507k 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:

DK 507k364069-14-7BacterialTopoisomeraseStreptococcus pneumoniaegram-positive bacteriaDNA gyrase subunit AGyrAgram-negative bacteriasepticemiarat urinary tract infection modelspneumococcal pneumoniamouse lungspenicillin-resistant Streptococcus pneumoniaeInhibitorinhibitorinhibit

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