5-Fluorocytosine

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Chemical Structure| 2022-85-7 同义名 : 5-氟胞嘧啶 ;Flucytosine; NSC 103805; Flucytosine, 5-fluorocytosine, Flucytosin, Ancobon, Ancotil; Ancotil; Ancobon; 5-FC; Ro 2-9915
CAS号 : 2022-85-7
货号 : A200898
分子式 : C4H4FN3O
纯度 : 97%
分子量 : 129.09
MDL号 : MFCD00006035
存储条件：

Pure form Keep in dark place, sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(123.94 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 6.5 mg/mL(50.35 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Flucytosine (5-FC, 5-Fluorocytosine) is a synthetic antimycotic compound. In combination with amphotericin B, 5-FC can be used to treat severe systemic mycoses, such as cryptococcosis, candidosis, chromoblastomycosis and aspergillosis. Moreover, 5-FC has been combined with newer azole antifungal agents; it also plays an important role in a new approach to the treatment of cancer. The severe side effects of 5-FC include hepatotoxicity and bone-marrow depression[3]. 5-FC half-life in the serum of 10 rabbits increased from 3.35 +/- 0.27 to 24.63 +/- 0.70 hr after experimentally induced acute renal failure. Concentrations of 5-FC in the cerebrospinal fluid of five patients ranged from 17 to 62 mug/ml and were 74.4 +/- 5.6% of simultaneously determined serum concentrations[4]. The 5FC-FCZ (fluconazole, FCZ) combination was antagonistic against Candida species, but for some Candida isolates synergism was found. For C. neoformans the interaction for both combinations was highly dependent on the tested isolate and the method used[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

7.75mL

1.55mL

0.77mL

38.73mL

7.75mL

3.87mL

77.47mL

15.49mL

7.75mL
参考文献

[1]St-Germain G. Impact of endpoint definition on the outcome of antifungal susceptibility tests with Candida species: 24- versus 48-h incubation and 50 versus 80% reduction in growth. Mycoses. 2001;44(1-2):37-45.

[2]Feldmesser M, Mukherjee J, Casadevall A. Combination of 5-flucytosine and capsule-binding monoclonal antibody in the treatment of murine Cryptococcus neoformans infections and in vitro. J Antimicrob Chemother. 1996 Mar;37(3):617-22.

[3]Vermes A, Guchelaar HJ, Dankert J. Flucytosine: a review of its pharmacology, clinical indications, pharmacokinetics, toxicity and drug interactions. J Antimicrob Chemother. 2000;46(2):171‐179

[4]Block ER, Bennett JE. Pharmacological studies with 5-fluorocytosine. Antimicrob Agents Chemother. 1972;1(6):476‐482

[5]Te Dorsthorst DT, Verweij PE, Meletiadis J, et al. In vitro interaction of flucytosine combined with amphotericin B or fluconazole against thirty-five yeast isolates determined by both the fractional inhibitory concentration index and the response surface approach. Antimicrob Agents Chemother. 2002;46(9):2982‐2989