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ZD7288  ≥98%

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包装规格：5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(50mg/ml超声)
产品描述：基本信息 产品编号： Z10075 产品名称： ZD7288 CAS: 133059-99-1   储存条件 粉末 -20℃ 四年     分子式： C15H21ClN4 溶于液体 -80℃ 6个月 分子量： 292.81 -20℃ 1个月 化学名：  4-Pyrimidinamine,N-ethyl-1,6-dihydro-1,2-dimethyl-6-(methylimino)-N-phenyl-,hydrochloride (1:1) Solubility (25°C)：   体外:   DMSO   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 3.4152mL 17.0759mL 34.1518mL 5mM 0.6830mL 3.4152mL 6.8304mL 10mM 0.3415mL 1.7076mL 3.4152mL   生物活性 产品描述 一种有选择性的超极化激活的环核苷酸门控(HCN)通道阻断剂。 靶点 HCN channel   体外研究 ZD7288 is a selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker.ZD7288 inhibits glutamate release in a concentration-dependent manner. After incubation with 1,5 and 50µM ZD7288 for 24 hours,glutamate content in extracellular fluid is decreased to 69.0±2.8%,31.4±2.0% and 4.4±0.3%,respectively (P<0.01,vs.DMEM/F12 group [100.2±4.2%]).After incubation with ZD7288 (25,50,or 100µM) for 20 minutes,50µM glutamate-induced [Ca2+]i rises are attenuated to 59.2±2.7%,41.4±2.3% and 21.0±1.4%,respectively glutamate (P<0.01,vs. 50µM glutamate group). 体内研究 Application of ZD7288 0.1µM at 5 minutes before high-frequency stimulation significantly decreases the amplitude of field excitatory postsynaptic potentials (fEPSPs),and this inhibitory effect is maintained throughout the recording period.Application of 0.1µM ZD7288 30 minutes after high-frequency stimulation almost completely reverses the established long-term potentiation (LTP).Following application of ZD7288 (0.1µM) 5 minutes before high-frequency stimulation,glutamate content is reduced to 74.9±8.0% (P<0.05,vs.normal saline group).Furthermore,application of 0.1µM ZD7288 30 minutes after high-frequency stimulation markedly decreases the glutamate content to 77.0%±9.4% (P<0.05,vs.normal saline group).   推荐实验方法(仅供参考) 细胞实验:   Primary hippocampal neurons are obtained from neonatal (1 to 2 day-old) Sprague-Dawley rats,and used in this study.The cells are incubated for 24 hours with ZD7288 (1,5,or 50µM),8-bromoadenosine cyclic adenosine monophosphate (8-BrcAMP,5 or 50µM),or forskolin (1 or 5µM),and the culture medium is collected for glutamate measurement.   动物实验:   Specific-pathogen-free adult male Sprague-Dawley rats,aged 10 weeks and weighing 200±20g are used in this study.For hippocampal administration of saline or drugs,a cannula is carefully inserted into the CA3 area with an introductory tube fixed parallel to the recording electrode,reaching 0.1 to 0.2mm higher than the electrode tip.To test the effects of blockers on the induction of long-term potentiation (LTP),0.1µM ZD7288 or the monovalent cation cesium (Cs+) is applied 5 minutes before high-frequency stimulation.To test the effects of blockers on the maintenance of LTP,ZD7288/Cs+ is slowly administered using an infusion/withdrawal pump 30 minutes after the high-frequency stimulation.
保存条件：-20℃

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