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temafloxacin hydrochloride

Names

[ CAS No. ]:
105784-61-0

[ Name ]:
temafloxacin hydrochloride

[Synonym ]:
1-(2,4-Difluorophenyl)-6-fluoro-7-(3-methyl-1-piperazinyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid hydrochloride (1:1)
3-Quinolinecarboxylic acid, 1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-, hydrochloride (1:1)
1-(2,4-difluorophenyl)-6-fluoro-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride (1:1)
UNII:OC5IGJ7J6I
6-Fluoro-1-(2,4-difluorophenyl)-1-4-dihydro-7-(3-methylpiperazin-1-yl)-4-oxo-3-quinoline-carboxylic acid hydrochloride
UNII-OC5IGJ7J6I
Omniflox (TN)
Temafloxacin HCl
(±)-1-(2,4-Difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid monohydrochloride
temafloxacin hydrochloride

Biological Activity

[Description]:

Temafloxacin (TMFX) hydrochloride is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin hydrochloride is well tolerated in lower respiratory and genitourinary tract infections[1][2].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Temafloxacin hydrochloride (0-64 µg/mL; 18-24 h) shows good antibacterial activity for gram-positive/negative bacteria, with MIC ranges of <0.004-0.5, 0.5-2 and 0.06-0.25 µg/mL for E. coli, P. aeruginosa, and S. aureus, respectively[1]. Cell Viability Assay[1] Cell Line: E. coli (16 strains), P. aeruginosa (13 strains), and S. aureus (17 strains) Concentration: 0-64 µg/mL Incubation Time: 18-24 h Result: Inhibited E. coli (16 strains), P. aeruginosa, and S. aureus with MIC ranges of <0.004-0.5 (MIC 90%=0.06, =0.06), 0.5-2 (MIC 90%=1, MIC 50%=1) and 0.06-0.25 µg/mL (MIC 90%=0.125, MIC 50%=0.125). MIC 90% and 50% means MIC for 90% and 50% of the isolates (unit: µg/mL).

[In Vivo]

Temafloxacin hydrochloride (6.25, 25, 100 mg/kg; p.o.; single) shows good inhibitory activity to murine pyelonephritis[1]. Temafloxacin hydrochloride (100 mg/kg; p.o. or s.c.; single) shows rapid gastrointestinal absorption, and has excellent tissue and body fluid penetration and concentration (except for central nervous system (CNS))[1]. Animal Model: Female CF-1 mice (20-25 g) (murine pyelonephritis model)[1]. Dosage: 6.25, 25, 100 mg/kg Administration: Orally; single. Result: Reduced the number of viable bacteria in the kidneys of mice. Animal Model: Female CF-1 mice (20-25 g)[1]. Dosage: 100 mg/kg Administration: Subcutaneously or orally; single. Result: 1.19Pharmacokinetic Parameters of Temafloxacin hydrochloride in Female CF-1 mice[1]. Cmax (µg/mL) AUC (µg/mL•h) T1/2 (h) % Urinary recovery SC (100 mg/kg) 25.2 86.6 3.4 25.3 PO (100 mg/kg) 13.5 57.4 1.3 9.1

[References]

[1]. Hardy DJ, et al. Comparative antibacterial activities of temafloxacin hydrochloride (A-62254) and two reference fluoroquinolones. Antimicrob Agents Chemother. 1987 Nov;31(11):1768-74.

[2]. Pankey GA. Temafloxacin: an overview. Am J Med. 1991 Dec 30;91(6A):166S-172S.

Chemical & Physical Properties

[ Boiling Point ]:
608.9ºC at 760 mmHg

[ Molecular Formula ]:
C21H19ClF3N3O3

[ Molecular Weight ]:
453.842

[ Flash Point ]:
322.1ºC

[ Exact Mass ]:
453.106689

[ PSA ]:
74.57000

[ LogP ]:
4.10010

[ Vapour Pressure ]:
1.11E-15mmHg at 25°C

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds