Pefloxacin Mesylate Dihydrate

製品コードS4119 バッチS411901

化学情報

	Synonyms	1589 RB,Pefloxacinium mesylate dihydrate	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₇H₂₀FN₃O₃.CH₄O₃S.2H₂O
	分子量	465.49	CAS No.	149676-40-4
Solubility (25°C)*	体外	Water	67 mg/mL (143.93 mM)
		DMSO	9 mg/mL (19.33 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Pefloxacin Mesylate Dihydrate (1589 RB,Pefloxacinium mesylate dihydrate) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.
in vitro	Pefloxacin like that of other quinolones mainly targets bacterial DNA gyrase (topoisomerase II) which is an essential bacterial enzyme with a variety of activities. Pefloxacin is a strongly bactericidal in a complex manner; the bactericidal effect has been described as 'biphasic' with a single rapidly killing effect followed by a paradoxical reduced killing phase in the presence of increased concentration; in bacterial cells incubated with Pefloxacin, non-replicative DNA synthesis (DNA repair), termed SOS response, is induced and SOS response prevents replication, blocking cell division and producing filarnentation. Thus the end result of the SOS response is harmful for the bacteria with morphological and biochemical disturbances. Pefloxacin is highly active against the Enterobacteriaceae (Citrobacter, Enterobacter, Klebsiella, Morganella, Proteus); the minimal inhibitory concentrations (MICs) of Pefloxacin for all genus and species of this family of bacteria ranges usually between 0.03 and 4 or 8 mg/L; against Salmonella, Shigella and Yersinia the MIC50/MIC90 are lower: 0.12/1.0, 0.06/0.06, 0.12/0.25 mg/L, respectively. The MICs of Pefloxacin for Gram- negative aerobic bacilli, such as Pseudomonas aeruginosa, Acinetobacter spp., Alcaligenes, Pseudomonas spp. , ranges from 1 to 4 mg/L. Gram-positive cocci Staphylococci including S. aureus and coagulase-negative staphylococci even resistant to other antibiotics are susceptible or moderately susceptible to Pefloxacin, with MICs in the range 0.125-0.5 mg/L. The MICs of Pefloxacin for Legionella pneumophila are moderately low (MIC50/MIC90:1.0/1.0mg/L); for Eikenella corrodens, Vibrio cholerae, the MICs are very low, whereas Helicobacter pylori, Listeria monocytogenes and Nocardia astero'ides are resistant to Pefloxacin, with MIC50 of 8 mg/L or more. Mycobacteria are moderately or not susceptible to Pefloxacin and most anaerobes are resistant to Pefloxacin. Mycoplasma spp and Chlamydiae are poorly susceptible to Pefloxacin (MIC50/MIC90: 2/8 mg/L) whereas Rickettsia conori and Coxiella burneti are susceptible at therapeutically achievable concentrations. ^[1]

製品説明

Pefloxacin Mesylate Dihydrate (1589 RB,Pefloxacinium mesylate dihydrate) is the third generation of fluoroquinolone class of antibacterials, which inhibits Topoisomerase II activity and DNA replication.

in vitro

Pefloxacin like that of other quinolones mainly targets bacterial DNA gyrase (topoisomerase II) which is an essential bacterial enzyme with a variety of activities. Pefloxacin is a strongly bactericidal in a complex manner; the bactericidal effect has been described as 'biphasic' with a single rapidly killing effect followed by a paradoxical reduced killing phase in the presence of increased concentration; in bacterial cells incubated with Pefloxacin, non-replicative DNA synthesis (DNA repair), termed SOS response, is induced and SOS response prevents replication, blocking cell division and producing filarnentation. Thus the end result of the SOS response is harmful for the bacteria with morphological and biochemical disturbances. Pefloxacin is highly active against the Enterobacteriaceae (Citrobacter, Enterobacter, Klebsiella, Morganella, Proteus); the minimal inhibitory concentrations (MICs) of Pefloxacin for all genus and species of this family of bacteria ranges usually between 0.03 and 4 or 8 mg/L; against Salmonella, Shigella and Yersinia the MIC50/MIC90 are lower: 0.12/1.0, 0.06/0.06, 0.12/0.25 mg/L, respectively. The MICs of Pefloxacin for Gram- negative aerobic bacilli, such as Pseudomonas aeruginosa, Acinetobacter spp., Alcaligenes, Pseudomonas spp. , ranges from 1 to 4 mg/L. Gram-positive cocci Staphylococci including S. aureus and coagulase-negative staphylococci even resistant to other antibiotics are susceptible or moderately susceptible to Pefloxacin, with MICs in the range 0.125-0.5 mg/L. The MICs of Pefloxacin for Legionella pneumophila are moderately low (MIC50/MIC90:1.0/1.0mg/L); for Eikenella corrodens, Vibrio cholerae, the MICs are very low, whereas Helicobacter pylori, Listeria monocytogenes and Nocardia astero'ides are resistant to Pefloxacin, with MIC50 of 8 mg/L or more. Mycobacteria are moderately or not susceptible to Pefloxacin and most anaerobes are resistant to Pefloxacin. Mycoplasma spp and Chlamydiae are poorly susceptible to Pefloxacin (MIC50/MIC90: 2/8 mg/L) whereas Rickettsia conori and Coxiella burneti are susceptible at therapeutically achievable concentrations. ^[1]

プロトコル(参考用のみ)

参考

[1] Bergogne-Bérézin E1. Int J Antimicrob Agents, 1991, 1(1), 29-4

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人間や獣医の診断であるか治療的な使用のためにでない。

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