福司氟康唑

生物活性靶点体外研究体内研究福司氟康唑试剂级价格

福司氟康唑

CAS号:194798-83-9
英文名:Fosfluconazole
中文名:福司氟康唑
CBNumber:CB71120322
分子式:C13H13F2N6O4P
分子量:386.25
MOL File:194798-83-9.mol

福司氟康唑化学性质

熔点 :223-224°
沸点 :701.5±70.0 °C(Predicted)
密度 :1.70±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO : 6.2 mg/mL (16.05 mM)
酸度系数(pKa) :1.44±0.10(Predicted)

福司氟康唑性质、用途与生产工艺

生物活性 Fosfluconazole是一种水溶性的fluconazole盐酸盐前体药物。Fluconazole是三唑抗真菌药物，用于治疗和组织表面的和系统性真菌感染。
靶点

Antifungal
体外研究

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.
体内研究

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.