| Identification | Back Directory | [Name]
ABT-492 | [CAS]
189279-58-1 | [Synonyms]
WQ3034
CS-711
CS-2335
ABT-492
RX-3341
Delafloxacin
Delafloxacinum
ABT492/ABT-492
ABT-492(WQ-3034)
ABT-492/Delafloxacin
Delafloxacin, ABT-492
Delafloxacin Impurity
Delafloxacin Free Acid
DELAFLOXACIN;RX-3341;WQ-3034;ABT492
DELAFLOXACIN;DELAFLOXACINUM;RX-3341;WQ-3034;ABT492;ABT 492
DELAFLOXACINUM; RX-3341; WQ-3034; ABT492; ABT 492; ABT-492;WQ3034;WQ 3034
1-(6-aMino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
1-(6-Amino-3,5-difluoro-2-pyridinyl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-3-quinolinecarboxylic acid
1-(6-Amino-3,5-difluoro-pyridin-2-yl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-quinolin-3-carboxylic acid
3-Quinolinecarboxylic acid, 1-(6-aMino-3,5-difluoro-2-pyridinyl)-8-chloro-6-fluoro-1,4-dihydro-7-(3-hydroxy-1-azetidinyl)-4-oxo-
3-(6-Amino-3,5-difluoro-pyridin-2-ylamino)-2-{2,5-difluoro-4-[3-(3-methyl-2-oxo-butyl)-cyclobutyl]-benzoyl}-acrylic acid ethyl ester | [Molecular Formula]
C18H12ClF3N4O4 | [MDL Number]
MFCD09955301 | [MOL File]
189279-58-1.mol | [Molecular Weight]
440.76 |
| Chemical Properties | Back Directory | [Melting point ]
238-241℃ | [Boiling point ]
698.5±55.0 °C(Predicted) | [density ]
1.796 | [storage temp. ]
2-8°C | [solubility ]
DMSO (Slightly), Methanol (Very Slightly, Heated, Sonicated) | [form ]
powder | [pka]
5.49±0.50(Predicted) | [color ]
white to beige | [CAS DataBase Reference]
189279-58-1 |
| Hazard Information | Back Directory | [Uses]
Delafloxacin is a potent agent and broad-spectrum anionic fluoroquinolone against Streptococcus pneumoniae and diverse group of pathogens. | [Biochem/physiol Actions]
Delafloxacin is a fluoroquinolone antibiotic active against both Gram-negative and Gram-positive bacteria such as MRSA. Delafloxacin targets both DNA gyrase and topoisomerase IV, inhibiting DNA synthesis. Unlike most fluoroquinolones, delafloxacin is weakly acidic, which increases its potency in an acidic environments such as those existing in inflammatory cells and in skin and soft tissue infections. Delafloxacin shows good activity against most fluoroquinolone-resistant strains. | [in vivo]
Delafloxacin (the total daily doses vary from 0.156 to 640 mg/kg/24 h, subcutaneous injection) is highly effective against S. aureus. Against all four strains are observed a decrease of 1.5 to 2.2 log10 CFU in organism burden from untreated controls at even the lowest dose studied, and for two strains (MW2 and R2527) there is net bactericidal activity at the lowest dose. At the maximal doses studied, there is a >4-log10 kill from initial burden for all S. aureus strains[1].
Delafloxacin (2.5, 10, 40, and 160 mg/kg; subcutaneous injection, 24 h) has moderate terminal elimination half-life (t1/2=0.68 h, 0.79 h, 0.69 h and 1.0 h for 2.5 mg/kg, 10 mg/kg, 40 mg/kg, and 160 mg/kg, respectively)[1]. | Animal Model: | Mice with a neutropenic murine lung infection model (four S. aureus , four S. pneumoniae, and four K. pneumoniae strains)[1] | | Dosage: | The total daily doses vary from 0.156 to 640 mg/kg/24 h | | Administration: | 0.03 to 160 mg/kg are administered every 6 h (q6h) to infected mice by subcutaneous injection | | Result: | Inhibited S. aureus strains ATCC 29213, ATCC 33591, MW2, R2527 with MICs of 0.008, 0.008, 0.004, and 0.004 mg/L, respectively.
Inhibited S. pneumoniae strains ATCC 10813, ATCC 49619, 145, and 1329 with MICs of 0.03, 0.125, 0.016, and 0.016 mg/L, respectively.
Inhibited K. pneumonia strains ATCC 43816, 4105, 4110, and 81-1260A with MICs of 0.06, 1, 0.5, and 0.06 mg/L, respectively. |
| Animal Model: | Neutropenic mice[1] | | Dosage: | 2.5, 10, 40, and 160 mg/kg; 0.2 mL | | Administration: | Subcutaneous injection; 24 h | | Result: | The maximum drug concentrations (Cmax) concentrations ranged from 2 to 71 mg/L. AUC0-∞ values ranged from 2.8 to 152 mg?h/L and were linear across the 2.5- to 160-mg dosing range. The elimination half-life (t1/2) ranged from 0.7 to 1 h. |
| [IC 50]
Quinolone | [storage]
Store at -20°C |
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