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Desmethyl Levofloxacin

Cat. No. M39069
Desmethyl Levofloxacin Structure
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Quality Control & Documentation
Biological Activity

Desmethyl Levofloxacin is a metabolite of Levofloxacin. Levofloxacin, a synthetic fluoroquinolone, is an antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.

Chemical Information
Molecular Weight 347.34
Formula C17H18FN3O4
CAS Number 117707-40-1
Form Solid
Solubility (25°C) DMSO 8 mg/mL (ultrasonic and warming)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Takashi Azuma et al. Sci Total Environ. Environmental fate of pharmaceutical compounds and antimicrobial-resistant bacteria in hospital effluents, and contributions to pollutant loads in the surface waters in Japan

[2] Negar Mohammadhosseini et al. Daru. Synthesis and antibacterial activity of novel levofloxacin derivatives containing a substituted thienylethyl moiety

[3] Wei-Jian Wang et al. Yao Xue Xue Bao. [HPLC-MS identification of degradation products of levofloxacin]

[4] Alireza Foroumadi et al. Arch Pharm (Weinheim). Synthesis and antibacterial activity of nitroaryl thiadiazole-levofloxacin hybrids

[5] A Hemeryck et al. Xenobiotica. Pharmacokinetics, metabolism, excretion and plasma protein binding of 14C-levofloxacin after a single oral administration in the Rhesus monkey

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