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Temafloxacin (hydrochloride) (Synonyms: A-62254)

Catalog No.GC10128

Temafloxacin (TMFX) hydrochloride is an orally active quinolone broad-spectrum antibacterial agent.

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Temafloxacin (hydrochloride) Chemical Structure

Cas No.: 105784-61-0

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5mg
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10mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

MIC90: less than or equal to 0.06 micrograms/mL respiratory pathogens

Temafloxacin is a fluoroquinolone antibiotic.

Fluoroquinolone antibiotic is an organonitrogen heterocyclic antibiotic with a quinolone or quinolone-like moiety and have a fluorine atom attached to the central ring system.

In vitro: The in-vitro activities of temafloxacin, ciprofloxacin, and ofloxacin against gram-negative bacteria were compared. The 90% minimal inhibitory concentrations (MIC90s) of temafloxacin for respiratory pathogens were less than or equal to 0.06 micrograms/mL. Temafloxacin was also active against bacterial agents of sexually transmitted diseases, such as Neisseria gonorrhoeae and Chlamydia trachomatis [1].

In vivo: Mixed aerobic-anaerobic infection was induced by i.p. implantation of gelatin capsules containing Bacteroides fragilis, Escherichia coli, and sterile rat faeces. Temafloxacin was found to be highly active with a 90.9% cure rate in comparison with no treatment, and as active as a combination of clindamycin and gentamicin. Temafloxacin at 12 mg/dose resulted in rise to serum concentrations exceeding the MIC values of both microorganisms for at least 8 h [2].

Clinical trial: Clinical studies showed that temafloxacin has improved activity against pneumococci. Eradication rates in acute exacerbations of chronic bronchitis collated from individual studies are 98% overall and 100% in pneumococcal infections. Moreover, eradication rates in smokers and the elderly illustrate significant advantages for temafloxacin. In pneumonia, a twice-daily temafloxacin regimen has given equivalent overall results to those of amoxycillin (84.6% vs 80%) [3].

References:
[1] Hardy DJ.  In vitro activity of temafloxacin against gram-negative bacteria: an overview. Am J Med. 1991 Dec 30;91(6A):19S-23S.
[2] Thadepalli H, Hajji M, Perumal VK, Chuah SK, Gollapudi S.  Evaluation of temafloxacin in a rat model of intra-abdominal abscess. J Antimicrob Chemother. 1992 Jun;29(6):687-92.
[3] Ball P. The role of temafloxacin in the community setting: an overview. J Antimicrob Chemother. 1991 Dec;28 Suppl C:121-30.

Chemical Properties

Cas No. 105784-61-0 SDF
Synonyms A-62254
Chemical Name 1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, monohydrochloride
Canonical SMILES CC1CN(C2=C(F)C=C(C(C(C(O)=O)=CN3C4=CC=C(F)C=C4F)=O)C3=C2)CCN1.Cl
Formula C21H18F3N3O3 • HCl M.Wt 453.8
Solubility ≤2mg/ml in DMSO;5mg/ml in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2036 mL 11.0181 mL 22.0361 mL
5 mM 0.4407 mL 2.2036 mL 4.4072 mL
10 mM 0.2204 mL 1.1018 mL 2.2036 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Reviews

Review for Temafloxacin (hydrochloride)

Average Rating: 5 ★★★★★ (Based on Reviews and 20 reference(s) in Google Scholar.)

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