The primary targets of pradofloxacin are DNA topoisomerase II (DNA gyrase) and topoisomerase IV, which are essential for bacterial DNA replication. The drug inhibits these enzymes by binding to their active sites and disrupting DNA strand breakage and rejoining processes [1]

- Antibacterial Activity: pradofloxacin exhibits potent activity against Gram-negative and Gram-positive bacteria, anaerobes, Mycoplasma spp., Rickettsia spp., and some intracellular pathogens (e.g., Mycobacterium spp.). Minimum inhibitory concentrations (MICs) are generally low, with activity superior to first- and second-generation fluoroquinolones against many strains. The bactericidal effect is concentration-dependent, with rapid bacterial killing observed at concentrations above the MIC [1]

- Pharmacokinetics: After oral administration in dogs and cats, pradofloxacin achieves peak plasma concentrations (Cmax) within 3.0 hours. Terminal half-life ranges from 5–10 hours, and accumulation is minimal with once-daily dosing. Free drug concentrations in plasma account for 63–71% of total concentration, facilitating penetration into tissues and abscesses [1]
- Clinical Efficacy: In clinical trials, pradofloxacin demonstrated efficacy in treating skin infections (wounds, abscesses), urinary tract infections, upper respiratory tract infections, and periodontal infections in dogs and cats. Bacteriological and clinical cure rates were comparable or superior to other approved antimicrobial agents [1]

Absorption: High oral bioavailability; rapid absorption after administration of tablets or suspensions [1]
- Distribution: Due to its high free concentration in plasma, it is widely distributed in tissues, including abscesses and ocular tissues [1]
- Metabolism: Primarily excreted unchanged via the kidneys; minimal liver metabolism [1]
- Excretion: Approximately 70-80% of the dose is excreted in the urine, and 10-20% in the feces [1]
- Half-life: 5-10 hours in dogs and cats [1]

Safety Overview: Pradofloxacin is well tolerated at clinical doses. Adverse reactions are rare and usually mild, including transient gastrointestinal disturbances (e.g., diarrhea) and reversible leukopenia in kittens. No significant hepatotoxicity or nephrotoxicity was observed in preclinical studies [1].
- Contraindications: Due to potential toxicity to cartilage, it should be avoided in juvenile and growing animals. Use with caution in cats with pre-existing renal impairment or central nervous system disease [1].

[1]. Pharmacokinetics, pharmacodynamics and therapeutics of pradofloxacin in the dog and cat. J Vet Pharmacol Ther. 2013 Jun;36(3):209-21.

Pradofloxacin is a third-generation fluoroquinolone antibiotic developed by Animal Health GmbH, a subsidiary of Bayer HealthCare AG. It was approved by the European Commission in April 2011 for the treatment of bacterial infections in dogs and cats. Indications: Dogs: Treatment of wound infections caused by susceptible strains of Staphylococcus intermedius (including Staphylococcus pseudointermedius); superficial and deep pyoderma caused by susceptible strains of Staphylococcus intermedius (including Staphylococcus pseudointermedius); acute urinary tract infections caused by susceptible strains of Escherichia coli and Staphylococcus intermedius (including Staphylococcus pseudointermedius); as adjunctive therapy to mechanical or surgical periodontal treatment for severe gingival and periodontal tissue infections caused by susceptible strains of anaerobic bacteria (e.g., Porphyromonas spp.). Cats: Treatment of acute upper respiratory tract infections caused by susceptible strains of Pasteurella multocida, Escherichia coli, and Staphylococcus intermedius (including Staphylococcus pseudointermedius).
Dogs: Treatment of skin and soft tissue infections caused by Gram-positive bacteria (usually Staphylococcus and Streptococcus) and Gram-negative bacteria (such as Escherichia coli, Pseudomonas, and Proteus), such as superficial and deep pyoderma and wound infections; treatment of urinary tract infections caused by Gram-negative bacteria (such as Enterobacteriaceae, such as Escherichia coli, Enterobacter, Klebsiella, and Proteus). Infections of the gingiva and periodontal tissues caused by Pseudomonas spp. and Gram-positive bacteria (usually Staphylococcus spp.); infections of the gingiva and periodontal tissues caused by anaerobic bacteria (e.g., Porphyromonas spp., Prevotella spp., Fusobacterium spp., Eikenella spp.) and carbon dioxide-loving bacteria (e.g., Capnocytophaga spp.); in cats: respiratory infections caused by Gram-negative bacteria (e.g., Pasteurella spp., Escherichia coli, and Pseudomonas spp.) and Gram-positive bacteria (e.g., Streptococcus spp. and Staphylococcus spp.). - Mechanism of action: It inhibits bacterial DNA synthesis by targeting topoisomerases II and IV, thereby preventing DNA replication and repair [1]
- Indications: It is approved for the treatment of skin infections, abscesses, urinary tract infections and respiratory infections in dogs and cats [1]
- Resistance: It has a lower tendency to develop resistance compared to older generation fluoroquinolones, as confirmed by mutation prevention concentration (MPC) assays [1]
- Dosage: Cats are given 7.5 mg/kg orally once daily for 7 days; dogs are given 3-5 mg/kg orally once daily for the treatment of various diseases [1]

C21H21N4O3F

396.41

396.16

C, 63.63; H, 5.34; F, 4.79; N, 14.13; O, 12.11

195532-12-8

9802884

Light yellow to yellow solid powder

1.504g/cm3

664.525ºC at 760 mmHg

355.692ºC

0mmHg at 25°C

1.691

2.627

2

8

3

29

803

2

C(C1=C2C(C(=O)C(C(O)=O)=CN2C2CC2)=CC(F)=C1N1CC2C(NCCC2)C1)#N

LZLXHGFNOWILIY-APPDUMDISA-N

InChI=1S/C21H21FN4O3/c22-16-6-13-18(26(12-3-4-12)9-15(20(13)27)21(28)29)14(7-23)19(16)25-8-11-2-1-5-24-17(11)10-25/h6,9,11-12,17,24H,1-5,8,10H2,(H,28,29)/t11-,17+/m0/s1

7-[(4aS,7aS)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-8-cyano-1-cyclopropyl-6-fluoro-4-oxoquinoline-3-carboxylic acid

Pradofloxacin; 195532-12-8; Veraflox; pradofloxacine; pradofloxacino; 6O0T5E048I; DTXSID60173229; pradofloxacinum;

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.)