Flucytosine
(Synonyms: 5-氟胞嘧啶; 5-Fluorocytosine; NSC 103805; Ro 2-9915) 目录号 : GC13753
A prodrug of 5-fluorouracil
Cas No.:2022-85-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
P. aeruginosa Strains |
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Preparation method |
The solubility of this compound in DMSO is >6.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
1, 4, 11, 33 and 100 μM; 14 h |
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Applications |
In P. aeruginosa strains, 5-Flucytosine (5-FC) inhibited pyoverdine synthesis and pvdE transcription. In a P. aeruginosa PAO1 fur mutant, 5-Flucytosine also inhibited pyoverdine production, suggesting that 5-FC could repress iron uptake genes through a Fur-independent mechanism. 5-Flucytosine down-regulated the expression of toxA and prpL genes, which was consistent with the strongly reduced ToxA and PrpL levels in culture supernatants, two major virulence factors of P. aeruginosa. |
| Animal experiment [1]: | |
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Animal models |
mouse model of pulmonary infection; mice infected with an isogenic pvdS mutant |
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Dosage form |
30 mg/kg per day; i.p. |
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Application |
In a mouse model of pulmonary infection with P. aeruginosa, 5-FC almost completely protected mice from the P. aeruginosa lethal challenge. All mice infected with the pvdS mutant survived the challenge, suggesting the importance of PvdS as a major pathogenicity determinant in P. aeruginosa pulmonary infection. 5-FC also reduced lesions and inflammation in bronchi and pulmonary parenchyma. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Imperi F1, Massai F, Facchini M, et al. Repurposing the antimycotic drug flucytosine for suppression of Pseudomonas aeruginosa pathogenicity. Proc Natl Acad Sci U S A. 2013 Apr 30;110(18):7458-63. | |
Flucytosine (5-Fluorocytosine, 5-FC, Ancobon), a fluorinated pyrimidine analogue, is an antifungal drug.Target: antifungalFlucytosine, or 5-fluorocytosine, a fluorinated pyrimidine analogue, is a synthetic antimycotic drug. It is structurally related to the cytostatic fluorouracil and to floxuridine. It is available in oral and in some countries also in injectable form. A common brand name is Ancobon. Flucytosine was first synthesized in 1957 but its antifungal properties were discovered in 1964. The drug is dispensed in capsules of 250 mg and 500 mg strength. The injectable form is diluted in 250 mL saline solution to contain 2.5 g total (10 mg/mL). The solution is physically incompatible with other drugs including amphotericin B.Flucytosine is well absorbed (75 to 90%) from the gastrointestinal tract. Intake with meals slows the absorption, but does not decrease the amount absorbed. Following an oral dose of 2 grams peak serum levels are reached after approximately 6 hours. The time to peak level decreases with continued therapy. After 4 days peak levels are measured after 2 hours. The drug is eliminated renally. In normal patients flucytosine has reportedly a half-life of 2.5 to 6 hours. In patients with impaired renal function higher serum levels are seen and the drug tends to cumulate in these patients. The drug is mainly excreted unchanged in the urine (90% of an oral dose) and only traces are metabolized and excreted in the feces. Therapeutic serum levels range from 25 to 100 g/ml. Serum levels in excess of 100 ug are associated with a higher incidence of side effects. Periodic measurements of serum levels are recommended for all patients and are a must in patients with renal damage.
References:
[1]. Vermes A, et al. Flucytosine: a review of its pharmacology, clinical indications, pharmacokinetics, toxicity and drug interactions. J Antimicrob Chemother. 2000 Aug;46(2):171-9.
[2]. Te Dorsthorst DT, 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 Sep;46(9):2982-9.
| Cas No. | 2022-85-7 | SDF | |
| 别名 | 5-氟胞嘧啶; 5-Fluorocytosine; NSC 103805; Ro 2-9915 | ||
| 化学名 | 6-amino-5-fluoro-1H-pyrimidin-2-one | ||
| Canonical SMILES | C1=NC(=O)NC(=C1F)N | ||
| 分子式 | C4H4FN3O | 分子量 | 129.09 |
| 溶解度 | ≥ 6.4mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 7.7465 mL | 38.7327 mL | 77.4653 mL |
| 5 mM | 1.5493 mL | 7.7465 mL | 15.4931 mL |
| 10 mM | 0.7747 mL | 3.8733 mL | 7.7465 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。