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Purity: ≥98%
Fosfluconazole is a water-soluble phosphate prodrug of fluconazole widely used as an antifungal agent. Fluconazole is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections.
| ln Vitro |
The apical or basal chamber of Transwell plates were supplemented with 10 μM fluconazole or fosphenytoin in order to investigate the polarized biotransformation and Transwell transit of phosphate prodrugs in Caco-2 monolayers. Both prodrugs were effectively cleaved in the apical chamber after two hours of incubation. Concentration-dependent ALP-mediated biotransformation was used to find the Michaelis-Menten constant (Km) for prodrug biotransformation in Caco-2 monolayers in order to investigate the kinetics of ALP-mediated biotransformation in more detail. For both fluconazole and fosphenytoin, saturation curves with increasing concentration were discovered. Fosphenytoin and fluconazole have estimated Km values of 1160 and 357 μM, respectively [2].
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| ln Vivo |
In intestinal mucosal fragments, the biotransformation of fluconazole appears to have an apparent half-life of 10 minutes [2]. An antifungal medication called fluconazole (FLCZ) works well to treat fungal peritonitis. The phosphate prodrug of fluconazole (F-FLCZ) has a greater solubility than FLCZ. Due to its high water solubility, F-FLCZ helps patients receiving continuous ambulatory peritoneal dialysis (CAPD) avoid fungal peritonitis. This work aimed to describe the pharmacokinetics of both FLCZ and F-FLCZ following intraperitoneal (ip) administration in peritoneal dialysis rats, as well as the peritoneal permeability of FLCZ. FLCZ, also known as F-FLCZ, is given intraperitoneally and intravenously. FLCZ was found in the dialysate and blood after peritoneal dialysis animals received F-FLCZ intraperitoneally. Following intravenous (iv) F-FLCZ injection, plasma FLCZ concentrations were higher than following intraperitoneal (ip) F-FLCZ administration. It is thought that when F-FLCZ is given intraperitoneally, the dosage should be suitably raised. A two-compartment model (peritoneal dialysis PK model) was used to examine the distribution of plasma FLCZ following intravenous and intraperitoneal dosing. The peripheral compartment's distribution volume was fixed to the dialysate volume. The distribution of dialysate FLCZ and plasma can be explained using the peritoneal dialysis PK model. These findings suggest that intraperitoneal administration of FLCZ and F-FLCZ can be used to treat fungal peritonitis in patients with CAPD [3].
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| References |
[1]. Hagiya H, et al. Successful treatment of recurrent candidemia due to candidal thrombophlebitis associated with a central venous catheter using a combination of Fosfluconazole and micafungin. Intern Med. 2013;52(18):2139-43.
[2]. Yuan H, et al. Evaluation of in vitro models for screening alkaline phosphatase-mediated bioconversion of phosphate ester prodrugs. Drug Metab Dispos. 2009 Jul;37(7):1443-7. [3]. Aoyama T, et al. Pharmacokinetics of fluconazole and Fosfluconazole after intraperitoneal administration to peritoneal dialysis rats. Drug Metab Pharmacokinet. 2005 Dec;20(6):485-90 |
| Additional Infomation |
Fosfluconazole is a member of triazoles, a triazole antifungal drug and a conazole antifungal drug. It has a role as a prodrug. It is functionally related to a fluconazole.
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| Molecular Formula |
C13H13F2N6O4P
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|---|---|
| Molecular Weight |
386.25
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| Exact Mass |
386.07
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| CAS # |
194798-83-9
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| Related CAS # |
194798-85-1 (sodium);194798-83-9 (free acid);
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| PubChem CID |
214356
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
701.5±70.0 °C at 760 mmHg
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| Flash Point |
378.1±35.7 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.684
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| LogP |
-1.23
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
26
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| Complexity |
511
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=C(C(CN2N=CN=C2)(OP(O)(O)=O)CN3N=CN=C3)C(F)=C1
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| InChi Key |
GHJWNRRCRIGGIO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H13F2N6O4P/c14-10-1-2-11(12(15)3-10)13(25-26(22,23)24,4-20-8-16-6-18-20)5-21-9-17-7-19-21/h1-3,6-9H,4-5H2,(H2,22,23,24)
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| Chemical Name |
[2-(2,4-difluorophenyl)-1,3-bis(1,2,4-triazol-1-yl)propan-2-yl] dihydrogen phosphate
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| Synonyms |
Fosfluconazole, Procif UK 292663 UK-292,663.
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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 |
| 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 : ~6.2 mg/mL (~16.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (16.18 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 62.5 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: ≥ 6.25 mg/mL (16.18 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 62.5 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: ≥ 6.25 mg/mL (16.18 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 | 2.5890 mL | 12.9450 mL | 25.8900 mL | |
| 5 mM | 0.5178 mL | 2.5890 mL | 5.1780 mL | |
| 10 mM | 0.2589 mL | 1.2945 mL | 2.5890 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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