| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Florfenicol metabolite
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|---|---|
| ln Vitro |
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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| References | |
| Additional Infomation |
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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| Molecular Formula |
C10H15CLFNO3S
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|---|---|
| Molecular Weight |
283.75
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| Exact Mass |
283.045
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| CAS # |
108656-33-3
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| Related CAS # |
Florfenicol amine;76639-93-5
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| PubChem CID |
19422964
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| Appearance |
White to off-white solid powder
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| Melting Point |
162-164ºC
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| LogP |
3.003
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
307
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.FC[C@H]([C@@H](C1C=CC(S(=O)(C)=O)=CC=1)O)N
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| InChi Key |
HWPBPTAOXVIKGI-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
2-amino-3-fluoro-1-(4-methylsulfonylphenyl)propan-1-ol;hydrochloride
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| Synonyms |
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;
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| HS Tariff Code |
2934.99.9001
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| Storage |
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. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 125 mg/mL (440.53 mM)
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|---|---|
| Solubility (In Vivo) |
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. 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. View More
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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5242 mL | 17.6211 mL | 35.2423 mL | |
| 5 mM | 0.7048 mL | 3.5242 mL | 7.0485 mL | |
| 10 mM | 0.3524 mL | 1.7621 mL | 3.5242 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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