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Tosufloxacin p-Toluenesulfonate Hydrate

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Tosufloxacin p-Toluenesulfonate Hydrate Basic information

Product Name:
Tosufloxacin p-Toluenesulfonate Hydrate
Synonyms:
  • Tosufloxacin (tosylate hydrate)
  • Tosufloxacin p-Toluenesulfonate Hydrate
  • 1,8-Naphthyridine-3-carboxylic acid, 7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-, 4-methylbenzenesulfonate, hydrate (1:1:)
  • A-61827 tosylate hydrate
  • T-3262 Tosylate Hydrate
  • Tosufloxacin tosylate hydrate (T3262, A61827)
  • Tosufloxacin tosylate hydrate, 10 mM in DMSO
  • Tosufloxacin toluenesulfonate hydrate - Bio-X ?
CAS:
1400591-39-0
MF:
C26H23F3N4O6S
MW:
576.55
Mol File:
1400591-39-0.mol
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Tosufloxacin p-Toluenesulfonate Hydrate Chemical Properties

storage temp. 
Store at -20°C
solubility 
DMSO : ≥ 33 mg/mL (55.50 mM)
form 
Solid
color 
White to off-white
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Safety Information

RTECS 
QN2791000
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Tosufloxacin p-Toluenesulfonate Hydrate Usage And Synthesis

Uses

Tosufloxacin tosylate hydrate (A-61827) is an orally active fluoroquinolone antibiotic. Tosufloxacin shows a broad spectrum of antibacterial activity against gram-positive and gram-negative bacteria[1][2].

Definition

ChEBI: A racemate comprising equimolar amounts of (R)- and (S)-tosufloxacin tosylate hydrate.

in vivo

Tosufloxacin tosylate hydrate (T-3262) (oral gavage; 0.16-13.39 mg/kg; once) treatment shows antibacterial activity against S. aureus, E. coli, and P. aeruginosa in vivo[2].

Animal Model:Male Slc:ICR mice infected with S. aureus[2]
Dosage:1.27-2.15 mg/kg
Administration:Oral gavage; 1.27-2.15 mg/kg; once
Result:Showed 50% effective dose (ED50) of 1.62 mg/kg (body weight) at 7 days after infection.
Showed MIC value of 0.0125 μg/mL.
Animal Model:Male Slc:ICR mice infected with E. coli[2]
Dosage:0.16-0.30 mg/kg
Administration:Oral gavage; 0.16-0.30 mg/kg; once
Result:Showed 50% effective dose (ED50) of 0.22 mg/kg (body weight) at 7 days after infection.
Showed MIC value of 0.0125 μg/mL.
Animal Model:Male Slc:ICR mice infected with P. aeruginosa[2]
Dosage:7.66-13.39 mg/kg
Administration:Oral gavage; 7.66-13.39 mg/kg; once
Result:Showed 50% effective dose (ED50) of 10.13 mg/kg (body weight) at 7 days after infection.
Showed MIC value of 0.78 μg/mL.

IC 50

Quinolone

References

[1] Chu DT, et al. Synthesis and biological properties of A-71497: a prodrug of tosufloxacin. Drugs Exp Clin Res. 1990;16(9):435-43. PMID:2100244
[2] Fujimaki K, et al. In vitro and in vivo antibacterial activities of T-3262, a new fluoroquinolone. Antimicrob Agents Chemother. 1988 Jun;32(6):827-33. DOI:10.1128/AAC.32.6.827

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