海恩酮  ≥98%

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包装规格:5mg 10mg in glass bottle
溶解性:溶于DMSO(12.5 mg/mL 超声)
产品描述:基本信息 产品编号:H10302 产品名称:Hycanthone CAS: 3105-97-3   储存条件 粉末 -20℃ 四年     分子式: C20H24N2O2S 溶于液体 -80℃ 六个月 分子量 356.48 -20℃ 一个月 化学名:  1-((2-(Diethylamino)ethyl)amino)-4-(hydroxymethyl)-9H-thioxanthen-9-one   Solubility (25°C)   体外 DMSO 10mg/mL (28.05mM; Need ultrasonic) Ethanol   Water   体内 现配现用   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.8052mL 14.0260mL 28.0521mL 5mM 0.5610mL 2.8052mL 5.6104mL 10mM 0.2805mL 1.4026mL 2.8052mL   生物活性 产品描述 一种噻吨酮类的 DNA 嵌入剂 (DNA intercalator),可抑制 RNA 合成以及 DNA 拓扑异构酶 I 和 II。 靶点/IC50 Topoisomerase I Topoisomerase II   体外研究 Hycanthone has an IC50 of 80nM for inhibition of APE1 incision of depurinated plasmid DNA. Hycanthone (0.05-100 µM; for 2 h) promotes APE1 cleavage in presence of Cycloheximide (CHX) and this cleavage is inhibited by 1% DMSO. Hycanthone at 20mg/mL or more is progressively more detrimental to cell viability. Results reveal that increased concentrations of Hycanthone, ranging from 0.1 to 10μg/mL, progressively reduces viral interferon yields as much as 73% compare to that of controls.   体内研究 Results show that the incorporation of tritiated thymidine into TCA-precipitable material of adult sensitive worms undergo a progressive decrease after treatment with Hycanthone. Immature worms are totally unaffected by Hycanthone at all times tested. Male worms treated with Hycanthone show signs of a possible partial recovery from the initial low levels of incorporation. The incorporation of tritiated leucine by drug-sensitive worms treated with Hycanthone is inhibited by 40 to 50% in the first four days after treatment. Results show that, 7 days after Hycanthone treatment, both ribosomal RNA species are reduced by at least 80% with respect to untreated worms, with some indication of a possible accumulation of heavier precursor molecules.   推荐实验方法(仅供参考) 细胞实验: Cell Assay Appropriate quantities of Hycanthone (1 to 100μg) in 10mL maintenance medium are added to plastic flasks (75cm2) containing approximately 3×107 LLC-MK2 cells in monolayer, which are then incubated at 35°C for 24h. Maintenance medium is decanted, and 2mL influenza virus is added onto cell monolayers and incubated at 35°C for 2h. The multiplicity of infection is approximately 1.0. Inoculum is removed and 10mL maintenance medium is added to each flask, which is then incubated at 35°C for 24h. Supernatant fluid is decanted, centrifuged at 100,000 g for 1 h, dialyzed against HCI-KCI buffer (pH 2.0) at 4°C for 24 h, and then dialyzed against two changes of phosphate-buffered saline (pH 7.1) at 4°C for 24h. Fluids are passed through filters to obtain sterile preparations. Samples are stored at -80°C until assayed for interferon activity.   动物实验:   Animal Administration Female outbred Swiss albino mice used as definitive hosts weigh 18 to 20 g at the time of infection. Hycanthone is administered at 0.01mL/g body weight intramuscularly by splitting the dose into the two hind legs, so that each mouse receives 80mg/kg body weight of the free base. Treatments are usually performed during the 8th week after infection.
保存条件:-20℃