|5-(3,4-二甲氧基苄基)嘧啶-2,4-二胺|CsnPharm

CAS No.: 5355-16-8

敌菌净 Catalog No. CSN21604

Synonyms: 二氨藜芦啶;EGIS-5645;敌菌净

Diaveridine is a dihydrofolate reductase (DHFR) inhibitor with Ki of 11.5 nM, also an antibacterial agent.

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技术信息

生物活性

描述Diaveridine is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent^[2]. A single oral administration of diaveridine significantly induced DNA damage in liver, kidney, lung, and spleen cells, but not in bone marrow cells. The significant increase in migration values of DNA was reproducible with dose-response relationship. Treatments with Diaveridine for 90 min have a strong bactericidal effect on S. typhimurium TA1535, and no bacterial growth is observed at 10μg/mL or more. Without metabolic activation, treatment with Diaveridine for 48 h, but not 24 h, causes a dose-dependent, significant increase in the frequency of aberrant metaphases. At 100 μg/mL, 60% of the metaphases contain chromosome aberrations^[3]. It is used in combination with sulfaquinoxaline as an antiprotozoal agent in animals for the prophylaxis and treatment of coccidiosis and leucocytozoonosis. In the acute oral toxicity tests, median lethal dose, LD50, was more than 2378mg/kg body weight in Sprague Dawley rats (1025mg/kg body weight in ICR mice). The testing results for three terms of mutagenicity toxicity (mouse chromosome aberration, erythrocyte micronucleus and sperm abnormality) were all negative at 128-512mg/kg body weight. For 90-day feeding of DVD (Diaveridine) at the dosage of 10mg/kg body weight in both male and female SD rats, no signs of toxicological effects were detected. Meanwhile, for teratogenicity test in female SD rats at the dosage of 37mg/kg body weight, there were no toxicological signs observed. Thus, our results suggested that the DVD is safe when administered orally in rats at 10mg/kg body weight per day^[4].
参考文献

[2] Sirichaiwat C, Intaraudom C, Kamchonwongpaisan S, Vanichtanankul J, Thebtaranonth Y, Yuthavong Y. Target guided synthesis of 5-benzyl-2,4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparum. J Med Chem. 2004 Jan 15;47(2):345-54
[3] Ono T, Sekiya T, Takahashi Y, Sasaki YF, Izumiyama F, Nishidate E, Tsuda S, Ohta T. The genotoxicity of diaveridine and trimethoprim. Environ Toxicol Pharmacol. 1997 Sep;3(4):297-306
[4] Wang J, Sun F, Tang S, Zhang S, Cao X. Acute, mutagenicity, teratogenicity and subchronic oral toxicity studies of diaveridine in rodents. Environ Toxicol Pharmacol. 2015 Sep;40(2):660-70

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8419 mL
- 19.2093 mL
- 38.4187 mL
- 5 mM
- 0.7684 mL
- 3.8419 mL
- 7.6837 mL
- 10 mM
- 0.3842 mL
- 1.9209 mL
- 3.8419 mL

技术信息

CAS号

5355-16-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H16N4O2

运输

蓝冰

分子量

260.29

别名

二氨藜芦啶;EGIS-5645;敌菌净

溶解度

DMSO	42.0 mg/mL (161.4 mM)
Water	20.0 mg/mL (76.8 mM)

动物实验配方

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