Fluorocytosine是抗真菌化合物。
产品描述
Flucytosine is a pyrimidine compound and a fluorinated cytosine analog exhibiting antifungal activity.
体外活性
在感染新型隐球菌的A/JCr小鼠中,Flucytosine和单抗2H1联合处理效果比单独给药效果好,明显降低肺部菌落形成.
体内活性
Lucytosine(≥1.25 mg / L)抑制Sabouraud葡萄糖培养液中C. neoformans的生长。
激酶实验
Microdilution method: The culture media used are RPMI 1640 with glutamine, without bicarbonate and phenol red, buffered with morpholinopropanesulfonic acid (MOPS) (0.165 M, pH 7.0). Two-fold serial dilutions of Flucytosine (0.06-64 μg/mL) are prepared and dispensed in 50 uL aliquot, in flat-bottom 96-well assay plates which are kept frozen at -70 °C in sealed plastic bags until used. The inoculum is prepared spectrophotometrically and standardized to a concentration of 1.0-5.0 × 103 cfu per mL. A 50 μL volume of this suspension is used to inoculate each well containing 50 μL of the double concentration of Flucytosine to be tested. Once inoculated, each well therefore contains 100 μL of broth favoured over 200 μL to facilitate the agitation of the plates prior to spectrophotometric reading. After an incubation period of 24 and 48 hours at 35 °C, the plates are agitated for 3 minutes at 900 r.p.m. with a shaker and the optical density of the growth in each well is determined with the use of an automatic plate reader set at 495 nm. The inhibitory concentration of IC50 is computed mathematically.
细胞实验
J774.16 murine macrophage-like cells plated on 96-well tissue culture plates are incubated with 500 u/mL murine recombinant gamma-interferon overnight at 37 °C. The medium is then replaced with fresh medium containing gamma-interferon 500 μ/mL, LPS 3 mg/L, C. neoformans cells 1.6 × 104/well and Flucytosine 50 mg/L. Plates are incubated for 24 hours at 37 °C. Cell supernatants are collected and cells lysed by adding 0.1 mL sterile distilled water to each well, incubating at room temperature for 30 minutes, and then aspirating and ejecting the lysate with a pipette several times to complete cell disruption. Wells are rinsed with PBS (0.1 mL) and the cell supernatant, and lysate and rinse from each well are pooled, vortexed, diluted 1:50, vortexed again and spread on Sabouraud's dextrose agar for the cfu determination(Only for Reference)
Cas No.
2022-85-7
分子式
C4H4FN3O
分子量
129.09
别名
Ro 2-9915;5-氟胞嘧啶;NSC 103805;Fluorocytosine;5-Fluorocytosine
储存和溶解度
DMSO:8 mg/mL (61.97 mM)
H2O:5 mg/mL (38.73 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years