Delafloxacin

SKU: orb1223213

Description

Delafloxacin (RX-3341, ABT-492) is a fluoroquinolone antibiotic agent. It has potent inhibitory against levofloxacin-resistant Streptococcus pneumoniae strains (MIC: 0.0078-0.125 μg/ml).

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 189279-58-1
• MW: 440.76
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₂ClF₃N₄O₄
• SMILES: C1C(CN1c1c(cc2c(c1Cl)n(cc(c2=O)C(=O)O)c1nc(c(cc1F)F)N)F)O
• Target: Wnt/beta/catenin
• Solubility: In Vitro: DMSO : 100 mg/mL (226.88 mM)

Bioactivity

• 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. 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). Animal model: Mice with a neutropenic murine lung infection model (fourS. aureus, four S. pneumoniae, and fourK. pneumoniae strains). 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. 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RX-3341 | WQ-3034 | ABT492

Quick Database Links

Gene Symbol

Wnt/beta/catenin