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Fosfluconazole

Fosfluconazole

产品编号 T5328   CAS 194798-83-9

Fosfluconazole 是 fluconazole 的水溶性磷酸盐前药。 它是一种抗真菌药物。

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Fosfluconazole Chemical Structure
Fosfluconazole, CAS 194798-83-9
规格 价格/CNY 货期 数量
5 mg ¥ 283 现货
10 mg ¥ 435 现货
25 mg ¥ 976 现货
50 mg ¥ 1,390 现货
100 mg ¥ 2,230 现货
200 mg ¥ 3,350 现货
1 mL * 10 mM (in DMSO) ¥ 357 现货
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
Venetoclax限时半价
MG-132限时半价
产品目录号及名称: Fosfluconazole (T5328)
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参考文献
产品描述 Fosfluconazole is water-soluble phosphate prodrug of fluconazole. Fluconazole is an antifungal drug.
体外活性 In Caco-2 monolayer, 10 μM Fosfluconazole 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. The rate of ALP-mediated conversion was prodrug concentration-dependent with Michaelis-Menten constants of 351 μM for fosfluconazole, determined in Caco-2 cells [1].
体内活性 Fosfluconazole was administered intravenously and intraperitoneally. After the i.p. administration of F-FLCZ, FLCZ was detected in circulating blood and the dialyzing fluid in peritoneal dialysis rats. The concentration of plasma FLCZ after the i.p. F-FLCZ administration was lower than that after the intravenous (i.v.) F-FLCZ administration [2].
激酶实验 An aliquot of 200 μl of mucosa scrap lysate solution was mixed with 100 mM phosphate buffer, pH 7.4, to a final volume at 1 ml. The concentration of the test compounds (fosphenytoin and fosfluconazole) was 10 μM. The incubation medium was prewarmed at 37°C before the reaction was initiated by addition of the tested compounds. An aliquot of 100 μl was collected from the incubation vial at the time points 0, 5, 10, 20, 30, 45, and 60 min and transferred to a 96-well plate, in which 100 μl of acetonitrile was prefilled to terminate the reaction. The samples were diluted 5-fold with acetonitrile containing 1 μM tolbutamide as an analytical internal standard. The samples were centrifuged at 4000 rpm for 5 min to precipitate protein. The supernatant was transferred to a new 96-well plate for concentration analysis by liquid chromatography/tandem mass spectrometry (LC/MS/MS) [1].
动物实验 Twelve-week-old male Wistar rats (200–300 g) were used. They were housed in a temperature-controlled room and were given food and water ad libitum. All rats were anesthetized by an i.p. administration of pentobarbital (50 mg/kg body weight). A catheter was placed in the peritoneal cavity and used as an inflow drain for the dialyzing fluid. sampling. In rats receiving i.v. administration, a catheter was inserted into the left jugular vein for drug administration, and another into the right femoral artery for blood sampling. Blood samples after the i.p. administration were obtained from the heart. The rats were then allowed to recover from the anesthesia and surgery for at least 24 hr. After the 40-mL dialyzing fluid was administered intraperitoneally, FLCZ 16 mg/kg body weight) and F-FLCZ (16 mg FLCZ eq/kg body weight) were administered intravenously. The volume of the drug solution administered intravenously was 8 mL/kg. FLCZ (16 mg/kg body weight) and F-FLCZ (16 mg FLCZ eq/kg body weight) dissolved in the 40 mL of dialyzing fluid were administered intraperitoneally. The dialyzing fluid FLCZ concentration was 100 mg/L. F-FLCZ (16 mg FLCZ eq/kg body weight) was administered to ARF rats intravenously and intraperitoneally. Blood (0.5 mL) and dialyzing ‰uid (1.5 mL) samples were collected at appropriate time intervals [2].
分子量 386.25
分子式 C13H13F2N6O4P
CAS No. 194798-83-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 6 mg/mL (15.53 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.589 mL 12.945 mL 25.89 mL 64.7249 mL
5 mM 0.5178 mL 2.589 mL 5.178 mL 12.945 mL
10 mM 0.2589 mL 1.2945 mL 2.589 mL 6.4725 mL

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TargetMol Library Books参考文献

1. 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. 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.
Dictamine Paclobutrazol Sulconazole mononitrate Amphotericin B 3-Carene Potassium gluconate Amorolfine hydrochloride Rapamycin

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抗真菌库 已知活性化合物库 FDA 上市药物库 含氟化合物库 FDA上市及药典收录分子库 经典已知活性库 NO PAINS 化合物库 免疫/炎症分子化合物库 上市药物库

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母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Fosfluconazole 194798-83-9 Microbiology/Virology Antifungal Fungal Inhibitor inhibit inhibitor

 

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