Florfenicol metabolite
Florfenicol amine hydrochloride targets bacterial protein synthesis through its parent compound florfenicol. Florfenicol inhibits bacterial protein synthesis by binding to 50S and 70S subunits in the ribosome to abolish the activity of peptidyltransferase. As a metabolite of florfenicol, florfenicol amine hydrochloride is used as a marker for florfenicol exposure and as a research tool for studying antibiotic metabolism and resistance. The compound has antimicrobial activity against various bacterial pathogens.

The pharmacokinetics of florfenicol and its metabolite, florfenicol amine, was investigated after its intravenous (i.v.) and oral (p.o.) administration of 20 mg/kg of body weight in Korean catfish (Silurus asotus). After i.v. florfenicol injection (as a bolus), the terminal half-life (t(1/2)), the volume of distribution at steady state (V(dss)), and total body clearance were 11.12 +/- 1.06 h, 1.09 +/- 0.09 L/kg and 0.07 +/- 0.01 L x kg/h respectively. After p.o. administration of florfenicol, the t(1/2), C(max), t(max) and oral bioavailability (F) were 15.69 +/- 2.59 h, 9.59 +/- 0.36 microg/mL, 8 h and 92.61 +/- 10.1% respectively. Florfenicol amine, an active metabolite of florfenicol, was detected in all fish. After i.v. and p.o. administration of florfenicol, the observed C(max) values of florfenicol amine (3.91 +/- 0.69 and 3.57 +/- 0.65 mg/L) were reached at 0.5 and 7.33 +/- 1.15 h. The mean metabolic rate of florfenicol amine after i.v. and p.o. administration was 0.4 and 0.5 respectively[1].

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Florfenicol amine hydrochloride demonstrates in vitro antimicrobial activity. It is a metabolite of florfenicol, which inhibits bacterial protein synthesis by binding to ribosomal subunits. The compound's activity is typically assessed in antimicrobial susceptibility testing against various bacterial strains including Bartonella, Edwardsiella, Escherichia coli, and Salmonella. It is used in research for studying antibiotic resistance and bacterial pathogenesis.

In vivo studies for Florfenicol amine hydrochloride are typically conducted in the context of veterinary medicine and aquaculture. The compound is a metabolite of florfenicol, a veterinary antibiotic used to control susceptible bacterial diseases in aquaculture and ranching. Studies in animals are used to evaluate the pharmacokinetics, tissue distribution, and elimination of florfenicol and its metabolites. The compound is not intended for human therapeutic use.

For antimicrobial susceptibility testing, Florfenicol amine hydrochloride is evaluated against bacterial strains using standard broth microdilution or agar diffusion methods. Serial dilutions of the compound are prepared in appropriate growth media and inoculated with standardized bacterial suspensions. Minimum inhibitory concentration (MIC) values are determined after incubation. For metabolism studies, the compound is analyzed by LC-MS or HPLC in biological samples.

For cellular studies, bacterial cultures are grown in appropriate media and treated with Florfenicol amine hydrochloride at various concentrations. Bacterial growth inhibition is assessed by measuring optical density or by colony counting. The compound's effects on bacterial protein synthesis can be assessed by measuring incorporation of radiolabeled amino acids. Cytotoxicity in mammalian cells can be assessed using standard cell viability assays for safety evaluation.

For in vivo studies, appropriate animal models are used to evaluate the pharmacokinetics and tissue distribution of florfenicol and its metabolite florfenicol amine hydrochloride. Animals are administered florfenicol via various routes, and blood, urine, and tissue samples are collected at various time points. Florfenicol amine hydrochloride concentrations are measured by LC-MS or HPLC. Efficacy against bacterial infections is evaluated in disease models.

Pharmacokinetic properties of Florfenicol amine hydrochloride are characterized as part of florfenicol metabolism studies. The compound has a molecular weight of 283.75 and purity ≥95%. It is a metabolite of florfenicol, which is used in veterinary medicine. The compound's pharmacokinetic properties include absorption, distribution, metabolism, and excretion of florfenicol and its metabolites. Comprehensive PK studies are available in the veterinary pharmacology literature.

Florfenicol amine hydrochloride is a research compound intended for laboratory use only and is not approved for human or veterinary therapeutic use. As a metabolite of florfenicol, it is used in research for studying antibiotic metabolism, pharmacokinetics, and resistance. The compound is widely used in aquaculture and ranching research. Standard laboratory safety precautions should be followed when handling this compound. Purity ≥95%.

[1]. Pharmacokinetics of florfenicol and its metabolite, florfenicol amine, in the Korean catfish (Silurus asotus). J Vet Pharmacol Ther. 2006 Feb;29(1):37-40.

[2]. Plasma and tissue depletion of florfenicol and florfenicol-amine in chickens. J Agric Food Chem. 2008 Nov 26;56(22):11049-56.

This study used chickens as a model to investigate the plasma drug distribution of florfenicol after a single intravenous (iv) and oral administration (20 mg/kg body weight), as well as the plasma residues of florfenicol and its main metabolite florfenicol after multiple oral administrations (40 mg/kg body weight, once daily for 3 consecutive days). High-performance liquid chromatography (HPLC) was used to analyze plasma and tissue samples. After both intravenous and oral administration, the plasma concentration-time curves conformed to a two-compartment open model. The mean elimination half-life (t1/2β) of florfenicol in plasma after intravenous and oral administration were 7.90 ± 0.48 h and 8.34 ± 0.64 h, respectively. The peak plasma concentration was 10.23 ± 1.67 μg/mL, and the time interval from oral administration to reaching the peak concentration was 0.63 ± 0.07 h. The oral bioavailability was 87 ± 16%. Florfenicol can be converted to florfenicol. Following multiple oral administrations (40 mg/kg body weight, once daily for 3 consecutive days), concentrations of florfenicol (119.34 ± 31.81 and 817.34 ± 91.65 μg/kg, respectively) and florfenicolamine (60.67 ± 13.05 and 48.50 ± 13.07 μg/kg, respectively) persisted in the kidneys and liver for 7 days. The long-term presence of florfenicol and florfenicolamine residues in edible tissues may pose a significant threat to human food safety due to the potential health risks associated with these compounds. A 6-day withdrawal period is required to ensure that florfenicol residues are below the maximum residue limits or permissible limits set by the European Union. [2]

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Florfenicol amine hydrochloride is a metabolite of the broad-spectrum antibiotic florfenicol with molecular weight 283.75 and purity ≥95%. It is used as a research tool for studying antibiotic metabolism, pharmacokinetics, and bacterial resistance. The compound is widely used in aquaculture and ranching research for studying diseases caused by various bacterial pathogens. It is for research use only and has not been approved for clinical applications.

C10H15CLFNO3S

283.75

283.045

108656-33-3

Florfenicol amine;76639-93-5

19422964

White to off-white solid powder

162-164ºC

3.003

3

5

4

17

307

0

Cl.FC[C@H]([C@@H](C1C=CC(S(=O)(C)=O)=CC=1)O)N

HWPBPTAOXVIKGI-UHFFFAOYSA-N

InChI=1S/C10H14FNO3S.ClH/c1-16(14,15)8-4-2-7(3-5-8)10(13)9(12)6-11;/h2-5,9-10,13H,6,12H2,1H3;1H

2-amino-3-fluoro-1-(4-methylsulfonylphenyl)propan-1-ol;hydrochloride

Florfenicol Amine Hydrochloride; 108656-33-3; 2-amino-3-fluoro-1-(4-methylsulfonylphenyl)propan-1-ol;hydrochloride; FLORFENICOL AMINE, HYDROCHLORIDE; Flufenicol impurities 3; SCHEMBL9177460; HWPBPTAOXVIKGI-UHFFFAOYSA-N;

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 : 125 mg/mL (440.53 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (7.33 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2.08 mg/mL (7.33 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 20.8 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: ≥ 2.08 mg/mL (7.33 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 20.8 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.)