Fosfluconazole|194798-83-9|(福司氟康唑)-陌孚医药/Medlife

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Fosfluconazole (Synonyms: 福司氟康唑)

目录号: PC19091 纯度: ≥98%

CAS No. :194798-83-9

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中文名称

Fosfluconazole

中文别名

2-(2,4-二氟苯基)-1,3-二(1H-1,2,4-三氮唑-1-基)丙基二氢磷酸酯;福司氟康唑;福司氟康唑杂质;磷氟康唑;磷氟康唑（福司氟康唑）;磷康唑;膦氟康唑

英文名称

Fosfluconazole

英文别名

1H-1,2,4-Triazole-1-ethanol, a-(2,4-difluorophenyl)-a-(1H-1,2,4-triazol-1-ylmethyl)-,1-(dihydrogen phosphate);[2-(2,4-difluorophenyl)-1,3-bis(1,2,4-triazol-1-yl)propan-2-yl] dihydrogen phosphate;1H-1,2,4-Triazole-1-ethanol, a-(2,4-difluorophenyl)-a-(1H-1,2,4-triazol-1-ylmethyl)-,1-(dihydr...;2-(2,4-difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propyl dihydrogen phosphate;Fosfluconazole;Procif;UNII-3JIJ299EWH;Prodif;Dihydrogen phosphate ester;PHARMA PRODUCT FLUCONAZOLE USP 2-(2,4-DIFLUOROPHENYL)-1,3-BIS(1,2,4-TRIAZOL-1-YL) PROPAN-2-OL;Fosfluconazole, >=98%

Cas No.

194798-83-9

分子式

C₁₃H₁₃N₆O₄F₂P

分子量

386.25

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Fosfluconazole is a prodrug of Fluconazole that is widely used as an antifungal agent.

性状

Solid

IC50 & Target[1][2]

Antifungal

体外研究(In Vitro)

To investigate the polarized bioconversion and the Transwell transport of phosphate prodrugs in Caco-2 monolayer, 10 μM Fosfluconazole or Fosphenytoin is dosed either in the apical or basal compartment in Transwell plates. Both prodrugs are efficiently cleaved in the apical compartment after a 2 h incubation. To further investigate the kinetics of ALP-mediated bioconversion, the concentration-dependent ALP-mediated bioconversions are conducted to determine the Michaelis-Menten constant (K_m) of prodrug bioconversion in Caco-2 monolayers. The saturation curves of Fosphenytoin and Fosfluconazole with the concentration increase are found. The estimated K_m values of Fosphenytoin and Fosfluconazole are 1160 and 357 μM, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

The apparent half-life for Fosfluconazole bioconversion in intestinal mucosa scraps is 10 min. Fluconazole (FLCZ) is an antifungal agent that is efficacious in the treatment of fungal peritonitis. Fosfluconazole (F-FLCZ) is the phosphate prodrug of FLCZ, which is highly soluble compared with FLCZ. F-FLCZ is useful against fungal peritonitis in continuous ambulatory peritoneal dialysis (CAPD) patients because it has a high water solubility. The aims of the present study are to characterize the peritoneal permeability of FLCZ and the pharmacokinetics of FLCZ and F-FLCZ after intraperitoneal (i.p.) administration to peritoneal dialysis rats. FLCZ or F-FLCZ is administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ is detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration is lower than that after the intravenous (i.v.) F-FLCZ administration. It is considered that the dose should be increased appropriately when F-FLCZ is administered intraperitoneally. The profiles of plasma FLCZ after i.v. and i.p. administrations are analyzed using a two-compartment model in which the distribution volume of the peripheral compartment is fixed at a volume of the dialyzing fluid (peritoneal dialysis PK model). The peritoneal dialysis PK model could describe the profiles of plasma and dialyzing fluid FLCZ. These results suggest that FLCZ and F-FLCZ could be administered intraperitoneally for the treatment of fungal peritonitis in CAPD patients.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[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. [Information]

[2]. Yuan H, et al. Evaluation of 体外研究 models for screening alkaline phosphatase-mediated bioconversion of phosphate ester prodrugs. Drug Metab Dispos. 2009 Jul;37(7):1443-7. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 6.2 mg/mL (16.05 mM; Need ultrasonic and warming)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 6.25 mg/mL (16.18 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (16.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 6.25 mg/mL (16.18 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (16.18 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6.25 mg/mL (16.18 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (16.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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