ChemicalBook CAS DataBase List 1400591-39-0

1400591-39-0

Name	Tosufloxacin p-Toluenesulfonate Hydrate
CAS	1400591-39-0
Molecular Formula	C19H15F3N4O3.C7H8O3S
MDL Number	MFCD01711971
Molecular Weight	576.544
MOL File	1400591-39-0.mol

Chemical Properties

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

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338
RTECS	QN2791000

Hazard Information

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

storage

Store at -20°C

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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