Lascufloxacin

CAS No. 848416-07-9

Lascufloxacin ( KRP-AM1977X )

Catalog No. M26275 CAS No. 848416-07-9

Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Lascufloxacin
  • Note
    Research use only, not for human use.
  • Brief Description
    Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections.
  • Description
    Lascufloxacin has the potential for various infectious diseases treatment, including lower respiratory tract infections.Lascufloxacin is a potent and orally active fluoroquinolone antibacterial agent. Lascufloxacin potently inhibits infections caused by various pathogens, including quinolone-resistant strains.(In Vitro):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 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.(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.]) .
  • Synonyms
    KRP-AM1977X
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Cereblon
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    848416-07-9
  • Formula Weight
    439.4
  • Molecular Formula
    C21H24F3N3O4
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    COc1c(N2C[C@@H](F)[C@@H](CNC3CC3)C2)c(F)cc2c1n(CCF)cc(C(O)=O)c2=O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Shibata N, et al. Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands. J Med Chem. 2018 Jan 25;61(2):543-575.
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