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Flucytosine (5-Fluorocytosine)

別名：5-FC, NSC 103805, Ro 2-9915

Flucytosine (5-Fluorocytosine) is an antifungal drug with IC50 of 0.93 μM in C. albicans.

Flucytosine (5-Fluorocytosine)化学構造

CAS No. 2022-85-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 25500 国内在庫あり
JPY 22000 国内在庫あり
JPY 29500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Flucytosine (5-Fluorocytosine)関連製品

Fungal阻害剤の選択性比較

生物活性

製品説明 Flucytosine (5-Fluorocytosine) is an antifungal drug with IC50 of 0.93 μM in C. albicans.
特性 First synthesized in 1957, and antifungal properties discovered in 1964.
In Vitro
In vitro Flucytosine inhibits the growth of C. neoformans in Sabouraud's dextrose broth at concentrations ≥ 1.25 mg/L, and Flucytosine of 50 mg/L causes a ~50% reduction in colony-forming unit (cfu)\ in the J774.16 killing assay with viability of J774.16 cells not affected measured by trypan blue exclusion. The combination of Flucytosine and IgGl monoclonal antibody to Cryptococcus neoformans capsular glucuronoxylomannan is more effective in reducing the numbers of C. neoformans colony-forming units in vitro with J774.16 murine macrophage-like cells than either agent alone. [2] The efficacy of Flucytosine (5FC) in combination with amphotericin B (AB) and fluconazole (FCZ) is studied against 35 yeast isolates, of which the 5FC-FCZ combination is antagonistic against Candida species, but for some Candida isolates synergism is found. [3]
Kinase Assay 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.
細胞実験 細胞株 J774.16 murine macrophage-like cell line
濃度 Dissolved in PBS, final concentration 50 mg/L
反応時間 24 hours
実験の流れ 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
In Vivo
In Vivo Administration of Flucytosine in combination with monoclonal antibody 2H1 to A/JCr mice infected with C. neoformans significantly reduces lung but not brain cfu, which is more effective than either agent alone. [2] The combination of intravenous Flucytosine in 0.9% saline (NaCl) and amphotericin B (AmB) provides synergistic antifungal activity and is associated with a lower incidence of nephrotoxicity than with AmB treatment alone. Infusion of Flucytosine (5-10 mg/kg/min) dissolved in 5% glucose into the renal artery of an in situ perfused kidney for 15 minutes increases renal blood flow (RBF) in the rat, and the renal vasodilatation persists for the duration of the Flucytosine infusion. [4]
動物実験 動物モデル Male Sprague-Dawley rats
投与量 5 mg/kg/min
投与経路 In situ renal perfusion at a rate of 0.13 mL/min

化学情報

分子量 129.09 化学式

C4H4FN3O
CAS No. 2022-85-7 SDF Download Flucytosine (5-Fluorocytosine) SDFをダウンロードする
Smiles C1=NC(=O)NC(=C1F)N
保管

In vitro
Batch:

DMSO : 13 mg/mL ( (100.7 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 7 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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