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产品价格:电议      采购度:1612      原产地:美洲
发布时间:2021/7/30 18:20:51 所属地区:上海 上海市
简要描述:
Fosfluconazole 是 Fluconazole 的前药,广泛用作抗真菌剂。
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CAS No. : 194798-83-9
MCE 站:Fosfluconazole
产品活性:Fosfluconazole 是 Fluconazole 的前药,广泛用作抗真菌剂。
研究领域:Anti-infection
作用靶点:Fungal
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 (Km) of prodrug bioconversion in Caco-2 monolayers. The saturation curves of Fosphenytoin and Fosfluconazole with the concentration increase are found. The estimated Km values of Fosphenytoin and Fosfluconazole are 1160 and 357 μM, respectively.
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.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Anti-Infection Compound Library | FDA-Approved Drug Library | Drug Repurposing Compound Library | Antifungal Compound Library | FDA Approved & Pharmacopeial Drug Library | Rapamycin | Ferrostatin-1 | Cycloheximide | Staurosporine | Resveratrol | Tunicamycin | Hygromycin B | Oligomycin A | Camptothecin | Amphotericin B | Nystatin | Calcimycin | Filipin complex | Mycophenolic acid | Idarubicin hydrochloride | Fluconazole | Ketoconazole | Itraconazole | Caspofungin Acetate | Oligomycin | Posaconazole | Toyocamycin | Voriconazole | Cerulenin | Ciclopirox olamine | Isavuconazole | Leptomycin B | Hyperoside | Terbinafine | Anidulafungin
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更新时间:2024/1/2 10:17:29
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