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Merck
CN

P0106

Sigma-Aldrich

Pefloxacin 甲磺酸酯 二水合物

别名:

3-Quinolinecarboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-, monomethanesulfonate, dihydrate, Pefloxacine monomethanesulfonate dihydrate, Pefloxacinium methanesulfonate dihydrate

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About This Item

线性分子式:
C17H20FN3O3 • CH4O3S • 2H2O
分子量:
465.49
EC 号:
MDL编号:
UNSPSC代码:
51102829
PubChem化学物质编号:
NACRES:
NA.76

表单

powder

质量水平

溶解性

H2O: 50 mg/mL

抗生素抗菌谱

Gram-negative bacteria
Gram-positive bacteria

作用机制

DNA synthesis | interferes
enzyme | inhibits

储存温度

2-8°C

SMILES字符串

O.O.CS(O)(=O)=O.CCN1C=C(C(O)=O)C(=O)c2cc(F)c(cc12)N3CCN(C)CC3

InChI

1S/C17H20FN3O3.CH4O3S.2H2O/c1-3-20-10-12(17(23)24)16(22)11-8-13(18)15(9-14(11)20)21-6-4-19(2)5-7-21;1-5(2,3)4;;/h8-10H,3-7H2,1-2H3,(H,23,24);1H3,(H,2,3,4);2*1H2

InChI key

LEULAXMUNMRLPW-UHFFFAOYSA-N

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一般描述

Chemical structure: fluoroquinolone

应用

Pefloxacin is a synthetic broad-spectrum fluoroquinolone antibiotic that is effective against most gram-negative and gram-positive bacteria. It is used to treat gonococcal urethritis and for gram-negative-bacterial infections in the gastrointestinal system and the genitourinary tract. Pefloxacin mesylate dihydrate has been used to induce achilles tendon toxicity in rodents. It′s cytotoxicity and uptake have been studied in primary cultures of rat hepatocytes.

生化/生理作用

Pefloxacin inhibits the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase is thought to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV is thought to be the primary target in gram-positive organisms. The inhibition of the topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. Therefore, DNA replication and transcription is inhibited . Pefloxacin is an analog of norfloxacin.
Pefloxacin is a synthetic fluoroquinolone that functions an antibacterial agent. It is an analog of norfloxacin.
Mode of Action: Pefloxacin prevents bacterial DNA replication by inhibiting DNA gyrase.
Antimicrobial spectrum: Pefloxacin is highly active against Staphylococcus aureus, E. coli, other enterobacteria, and Pseudomonas aeruginosa. Active against gram-positive bacteria and excellent activity against gram-negative bacteria.

其他说明

Keep container tightly closed in a dry and well-ventilated place.

象形图

Exclamation mark

警示用语:

Warning

危险声明

预防措施声明

危险分类

Eye Irrit. 2

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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P Nordmann et al.
The Journal of antimicrobial chemotherapy, 24(3), 355-363 (1989-09-01)
The cytotoxicity and the uptake of three 4-quinolones--pefloxacin, ciprofloxacin, and ofloxacin--were investigated in primary cultures of rat hepatocytes. As assessed by intracellular enzyme release in culture media, pefloxacin at concentration 400 mg/l and ciprofloxacin at 200 mg/l were found to
M A Simonin et al.
Antimicrobial agents and chemotherapy, 44(4), 867-872 (2000-03-18)
Despite a relatively low incidence of serious side effects, fluoroquinolones and the fluoroquinolone pefloxacin have been reported to occasionally promote tendinopathy that might result in the complication of spontaneous rupture of tendons. In the present study, we investigated in rodents

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