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Lascufloxacin

CAS No. : 848416-07-9

MCE 站：Lascufloxacin

产品活性：Lascufloxacin (KRP-AM1977X) 是一种有效的口服活性的氟喹诺酮类抗菌剂。Lascufloxacin 有效抑制由多种病原体 (包括对喹诺酮类耐药的菌株) 引起的感染。Lascufloxacin 可用于多种传染病的研究，包括下呼吸道感染。

研究领域：Anti-infection

作用靶点：Bacterial

In Vitro: In the Gram-negative bacteria, Lascufloxacin shows antibacterial activities against Moraxella catarrhalis and β-lactamase-negative ampicillin-susceptible and ampicillin-resistant strains of Haemophilus influenzae, with an MIC₉₀ value of 0.06 μg/mL in all cases. The MIC₉₀ values against Enterobacter spp., Klebsiella pneumoniae, and Acinetobacter spp. are 0.25 μg/mL, 0.25 μg/mL, and 0.5 μg/mL, respectively. Lascufloxacin inhibits E. coli and P. aeruginosa with MIC₉₀s of 0.25 μg/mL and 4 μg/mL, respectively. The MIC₅₀ and MIC₉₀ values of Lascufloxacin against M. pneumoniae are 0.12 μg/mL and 0.25 μg/mL, respectively. Lascufloxacin shows potent activity against macrolide-resistant M. pneumoniae isolates with an MIC₉₀ of 0.12 μg/mL.
The MICs of Lascufloxacin against parent S. aureus strains ranged from 0.008 to 0.015 μg/mL, and those against fourth-step parC, gyrA, parC, and gyrA mutant strains are all 2 μg/mL. Lascufloxacin shows incomplete cross-resistance against the mutant strains. The activities of Lascufloxacin against first- and second-step mutant strains of S. pneumoniae are more potent than the activities of other quinolones, and the MICs of Lascufloxacin against gyrA and parC double mutants are 0.25 to 0.5 μg/mL.

In Vivo: A pharmacodynamic study using a mouse thigh infection model indicates that the ratios of the free area under the curve (fAUC) to MIC in plasma required for bacteriostasis, or 1-log or 2-log CFU killing against S. pneumoniae isolates, are 10, 16, and 28, respectively. Lascufloxacin shows significant bacterial killing in the mouse model when emulated the area under the concentration-time curve (AUC) in plasma in dose of 75 mg per day [q.d.]) .

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