Absorption, Distribution and Excretion
Good oral absorption. Metabolism/Metabolites Metabolized in the liver. Major metabolites are pefloxacin N-oxide and norfloxacin. Biological Half-Life 8.6 hours

Protein Binding
20-30%

[1].Drlica K, et al. DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92.

[2].Hussy P, et al. Effect of 4-quinolones and novobiocin on calf thymus DNA polymerase alpha primase complex, topoisomerases I and II, and growth of mammalian lymphoblasts. Antimicrob Agents Chemother. 1986 Jun;29(6):1073-8

Pefloxacin is a quinolone antibiotic with the structure 4-oxo-1,4-dihydroquinoline, substituted at positions 1, 3, 6, and 7 with ethyl, carboxyl, fluorine, and 4-methylpiperazin-1-yl groups, respectively. It possesses anti-infective, DNA synthesis inhibitory, and antibacterial activities. It is a quinolone, N-arylPecazine, N-alkylPecazine, quinolone antibiotic, fluoroquinolone antibiotic, and monocarboxylic acid compound. Pefloxacin is a synthetic broad-spectrum fluoroquinolone antibacterial agent effective against most Gram-negative and Gram-positive bacteria. Pefloxacin is a fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Pefloxacin inhibits the activity of microbial DNA gyrase and topoisomerase IV. This interferes with DNA replication and prevents cell division. A synthetic broad-spectrum fluoroquinolone antibacterial agent effective against most Gram-negative and Gram-positive bacteria. Indications Pefloxacin is used to treat uncomplicated gonococcal urethritis in men and Gram-negative bacterial infections of the gastrointestinal and genitourinary tracts. Mechanism of Action Pefloxacin's bactericidal action stems from its interference with the activity of bacterial DNA gyrase and topoisomerase IV, both essential for bacterial DNA transcription and replication. DNA gyrase appears to be the primary target of quinolone drugs against Gram-negative bacteria. Topoisomerase IV appears to be its preferred target against Gram-positive bacteria. Interference with these two topoisomerases leads to bacterial chromosome strand breaks, supercoiling, and rejoining. As a result, DNA replication and transcription are inhibited. Pharmacodynamics Pefloxacin is a fluoroquinolone antibiotic. Fluoroquinolones, including pefloxacin, exhibit excellent antibacterial activity against Gram-negative aerobic bacteria (such as Escherichia coli and Neisseria gonorrhoeae) and Gram-positive bacteria (including Streptococcus pneumoniae and Staphylococcus aureus). They also have effective antibacterial activity against Shigella, Salmonella, Campylobacter, Neisseria gonorrhoeae, as well as multidrug-resistant Pseudomonas and Enterobacteriaceae.

C17H20FN3O3

333.3634

333.148

70458-92-3

Pefloxacin mesylate;70458-95-6;Pefloxacin-d5;1228182-51-1;Pefloxacin-d3;2733455-58-6;Pefloxacin mesylate dihydrate;149676-40-4

51081

White to off-white solid powder

1.3±0.1 g/cm3

529.1±50.0 °C at 760 mmHg

273.8±30.1 °C

0.0±1.5 mmHg at 25°C

1.594

1.51

1

7

3

24

545

0

O=C(C1=CN(CC)C2=C(C=C(F)C(N3CCN(C)CC3)=C2)C1=O)O

FHFYDNQZQSQIAI-UHFFFAOYSA-N

InChI=1S/C17H20FN3O3/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/h8-10H,3-7H2,1-2H3,(H,23,24)

1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)-4-oxoquinoline-3-carboxylic acid

1589 RB 1584RB Pefloxacin

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)