Bacterial DNA gyrase (topoisomerase II) – Fluoroquinolone antibiotic that inhibits bacterial DNA replication [2]
Edwardsiella ictaluri – Bactericidal antibacterial agent effective against this catfish pathogen [2]

- Sarafloxacin is a potent antibacterial with minimum inhibitory concentrations (MICs) of ≤0.1 μg/mL against many important animal health pathogens (gram-negative bacteria); several gram-positive bacteria were found to be less sensitive, and fungi were not inhibited [1]
- Sarafloxacin demonstrated stability in extraction solvents (acetonitrile:water, 1:1, v/v; and pipermidic acid:KOH solution) with no degradation observed when standard was exposed to these solvents [1]
- In soil extraction studies, ACN:H₂O extractable radioactivity of ¹⁴C-sarafloxacin was less than 1% of applied radioactivity [1]
- HPLC analysis of ACN:H₂O extracts showed several components, all less than 1% of applied radioactivity; PIP:KOH extracts showed two major components: a polar component (retention time ~4-5 min) and unchanged sarafloxacin (retention time ~35 min) [1]
- The polar degradation component was acid-hydrolyzable and converted back to sarafloxacin when extracts were subjected to acid hydrolysis (2 N HCl, 60°C for 10 min) [1]
- Sarafloxacin was recovered intact from extracts of pure sand spiked with ¹⁴C-sarafloxacin, with little or no transformation observed [1]
- Sterile soils showed similar HPLC component profiles to nonsterile soils, indicating that transformation of sarafloxacin is an abiotic, soil-related phenomenon [1]

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Sarafloxacin (hydrochloride) is an antibiotic classified as a fluoroquinolone that is approved to treat illnesses in poultry. The results of the test indicated that the mineralization rates of 14CO2 in soil, silt soil, and sandy soil were, respectively, 0.58%, 0.49%, and 0.57% after the application of Sarafloxacin hydrochloride treatment [1]. Sarafloxacin hydrochloride's amount of inhibition on test cells varied. Sarafloxacin hydrochloride concentrations in broth seemed to affect E. Coli isolates five times less than in the simulated culture model, indicating that sarafloxacin might be partially inaccessible because of the model's consumption of organic matter [2].

- In three field trials with channel catfish naturally infected with Edwardsiella ictaluri, sarafloxacin administered in feed for 5 days at 10 or 12.5 mg/kg of fish significantly improved survival (P < 0.05) compared to nonmedicated controls [2]
- Trial 1: Nonmedicated survival 43%, sarafloxacin-medicated (12.5 mg/kg) survival 68%; weight gain was significantly higher (3.9 g vs 2.3 g, P < 0.05) [2]
- Trial 2: Nonmedicated survival 11%, sarafloxacin-medicated (10 mg/kg) survival 48%; survival difference significant (P < 0.05) regardless of survival equation used [2]
- Trial 3: Nonmedicated survival 59%, sarafloxacin-medicated (10 mg/kg) survival 73%, Romet-medicated (100 mg/kg, twice recommended dose) survival 82%; both medicated groups had significantly higher survival and weight gain than nonmedicated controls (P < 0.05) [2]
- In trial 3, fish fed sarafloxacin-medicated feed gained 6.9 g (range 6.3-7.4 g) compared to 5.8 g for nonmedicated fish, representing approximately 8% higher final weight [2]
- In trial 1, weight gain was 40% higher in medicated fish, representing approximately 10% higher final weight [2]
- Of concern, increased mortality was observed during the last days of trials 2 and 3 in fish that had received sarafloxacin-medicated feed 11-14 days earlier [2]
- In soil biodegradation study, mineralization of ¹⁴C-sarafloxacin to ¹⁴CO₂ was low: 0.58% in loam soil (80 days), 0.49% in silt loam soil (73 days), and 0.57% in sandy loam soil (66 days) [1]
- Organic volatiles were less than 0.01% of applied radioactivity [1]

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Sarafloxacin hydrochloride (hydrochloride) was shown to be successful in treating E. coli in each of the three field experiments. added to fish feed for five days at a dose of 10 or 12.5 mg/kg of ictaluri-infected solutions. In Trial 1, Trial 2, and Trial 3, the nongroup drug mean was 43%, 11%, and 59%, respectively. For the drug group using sarafloxacin hydrochloride, the equivalent averages were 68%, 48%, and 73%. In every trial, sarafloxacin hydrochloride was used as an antibiotic, and it significantly (P 0.05) increased survival [3].

- Soil biodegradation study: Three soil types (loam, silt loam, sandy loam) with varying organic matter content (5.8%, 2.5%, 1.3% respectively). Approximately 50 g (dry weight equivalent) of soil per flask. ¹⁴C-sarafloxacin hydrochloride (specific activity 55.6 mCi/mmol or 131.8 μCi/mg) was applied at 26.52 μCi or 0.20 mg per 50 g soil (4 μg/g soil). Unlabeled glucose (~10 mg carbon per 50 g soil) was added as carbon source. Soils were incubated in the dark at 22 ± 3°C. Trapping solutions were collected at 3, 5, 7, 14, 28, 42, 56 days and at termination (sandy loam: day 66, silt loam: day 73, loam: day 80). Water was added to maintain soils at 50-70% field capacity [1]
- Field trial 1: Six 0.9 m square polyethylene net-pens (0.6 cm mesh) in earthen pond (0.9 m depth). Channel catfish fingerlings (10-13 cm, average 12 g), 150 fish per pen. Medicated feed contained 500 mg sarafloxacin/kg feed. Fish fed at 2.5% body weight (resulting in 12.5 mg sarafloxacin/kg fish) for 5 consecutive days. Nonmedicated controls fed same rate. After 5-day treatment, all fish fed nonmedicated feed at 3% body weight for 14 days. Fish counted and weighed at termination [2]
- Field trial 2: 0.40 hectare pond (1.2 m depth). Twelve net-pens (diameter 1.2 m, depth 1.2 m, 0.6 cm mesh). Channel catfish fingerlings (7-11 cm, average 6.8 g), 200 fish per pen. Medicated feed containing 500 mg sarafloxacin/kg fed at 2% body weight (10 mg/kg fish) for 5 days. Nonmedicated controls fed same rate. Treatment initiated when first E. ictaluri-related death confirmed. After 5-day treatment, all fish fed nonmedicated feed at 3% body weight for 14 days [2]
- Field trial 3: Six 0.06 hectare ponds (1.2 m depth). Three net-pens (2.4 × 1.2 × 1.2 m, 0.6 cm mesh) per pond. Channel catfish fingerlings (7-10 cm, average 6.5 g), 250 fish per pen. Treatments: sarafloxacin-medicated feed (500 mg/kg, 2% body weight = 10 mg/kg fish), Romet-medicated feed (sulfadimethoxine-ormetoprim, 100 mg/kg fish, twice recommended dose), or nonmedicated feed. Fed for 5 consecutive days. Disease transmission ensured by adding naturally infected fish (~3,000 per pond) and immersion in 10,000 E. ictaluri cells/mL for 60 seconds [2]
- Soil extraction procedure: Soils extracted with acetonitrile:water (1:1, v/v), centrifuged at 3,000-3,500 rpm for 10 min. Supernatant decanted. Soil pellets further extracted with pipermidic acid:KOH (400 mg:1 mL of 1 N KOH). First extraction with 100 mL shaking overnight, subsequent extractions with 50 mL for 2 hours. Pooled extracts analyzed by HPLC [1]
- Soil combustion: After PIP:KOH extraction, soil residues air-dried, homogenized, and triplicate aliquots oxidized to determine radioactivity bound to soil [1]
- HPLC analysis conditions: Nucleosil C18 column (150 × 4.6 mm, 5 μm particle size); flow rate 1.0 mL/min; mobile phase A: 0.1% trifluoroacetic acid (aq), mobile phase B: acetonitrile:methanol (60:40, v/v); gradient elution; detection at 280 nm; radioactivity detector with 600 μL liquid cell [1]
- Acid hydrolysis: Equal volumes of PIP:KOH extracts and 2 N HCl mixed in vials, heated at 60°C for approximately 10 minutes, then analyzed by HPLC [1]

- Sarafloxacin hydrochloride is a fluoroquinolone antibiotic (molecular formula: C₃₈H₁F₁N₁O₃•HCl; molecular weight: 421.84; CAS registry number: 91296-87-6) registered for use against poultry diseases and tested for treatment of Edwardsiella ictaluri infections in channel catfish [1][2]
- The compound is a potent antibacterial with MICs ≤0.1 μg/mL against many gram-negative animal health pathogens [1]
- Sarafloxacin is a quinoline-3-carboxylic acid derivative: 1-(p-fluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-7-(piperazinyl)-quinoline-3-carboxylic acid [1]
- In soil, sarafloxacin strongly binds to organic matter; extractability decreased with increasing organic matter content: 25% in loam (5.8% OM), 73% in silt loam (2.5% OM), 81% in sandy loam (1.3% OM) using PIP:KOH extraction [1]
- The polar degradation component formed in soil is acid-hydrolyzable and converts back to sarafloxacin, suggesting reversible binding or complex formation [1]
- Formation of the polar component appears to be surface-catalyzed (clay, organic matter, or metals), not biologically mediated [1]
- In field trials, Romet (sulfadimethoxine-ormetoprim) at twice recommended dose (100 mg/kg) showed numerically higher survival (82%) compared to sarafloxacin (73%), but this difference was not significant in all survival calculations [2]
- Antibiotic resistance in E. ictaluri is an emerging concern: in 1990, 12 isolates resistant to oxytetracycline, 43 resistant to Romet, and 60 resistant to both were identified [2]

- Sarafloxacin was not toxic to soil microorganisms; bacterial populations were ≥5 × 10⁶ CFUs/g dry weight of soil at initiation and termination of the 80-day study in all three soils, confirming that sarafloxacin did not inhibit microbial growth [1]
- No adverse effects on fish were reported from sarafloxacin treatment in field trials; however, increased mortality was observed in the last days of trials 2 and 3 in sarafloxacin-treated groups [2]
- No LD50, hepatotoxicity, nephrotoxicity, or other detailed toxicity parameters were described for sarafloxacin in these papers [1][2]

[1]. Aerobic biodegradation of (14C)-sarafloxacin hydrochloride in soil. Environmental Toxicology and Chemistry, 1997. 16(3): p. 462-471.

[2]. Effects of sarafloxacin hydrochloride on human enteric bacteria under simulated human gut conditions. Vet Q, 1995 Mar;17(1):1-5.

[3]. Field efficacy trials of the antibacterial sarafloxacin-hydrochloride (A-56620) for treatment of Edwardsiella ictaluri infections in channel catfish. Journal of aquatic animal health, 1992. 4(4): p. 244-251.

Sarafloxacin hydrochloride belongs to the quinoline class of drugs.

C20H18CLF2N3O3

421.82

421.1

C, 56.95; H, 4.30; Cl, 8.40; F, 9.01; N, 9.96; O, 11.38

91296-87-6

Sarafloxacin;98105-99-8;Sarafloxacin-d8 hydrochloride trihydrate

56207

White to off-white solid powder

1.4±0.1 g/cm3

621.4±55.0 °C at 760 mmHg

275ºC

329.6±31.5 °C

0.0±1.9 mmHg at 25°C

1.633

2.09

3

8

3

29

645

0

C1CN(CCN1)C2=C(C=C3C(=C2)N(C=C(C3=O)C(=O)O)C4=CC=C(C=C4)F)F.Cl

KNWODGJQLCISLC-UHFFFAOYSA-N

InChI=1S/C20H17F2N3O3.ClH/c21-12-1-3-13(4-2-12)25-11-15(20(27)28)19(26)14-9-16(22)18(10-17(14)25)24-7-5-23-6-8-24;/h1-4,9-11,23H,5-8H2,(H,27,28);1H

6-fluoro-1-(4-fluorophenyl)-4-oxo-7-piperazin-1-ylquinoline-3-carboxylic acid;hydrochloride

A-56620; Sarafloxacin Hydrochloride; A 56620; A56620 HYDROCHLORIDE; 91296-87-6; Sarafloxacin HCl; Sarafin; SaraFlox WSP; A-56620n HCl

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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

DMSO : ~8.33 mg/mL (~19.75 mM)
H2O : ~1 mg/mL (~2.37 mM)

Solubility in Formulation 1: ≥ 0.83 mg/mL (1.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 0.83 mg/mL (1.97 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
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.

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Solubility in Formulation 3: ≥ 0.83 mg/mL (1.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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