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RWJ-51204  ≥98%

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包装规格：1mg in glass bottle
产品描述：基本信息 产品编号： R10366  产品名称： RWJ-51204 CAS: 205701-85-5   储存条件 粉末 -20℃ 四年 分子式： C21H19F2N3O3 溶于液体 -80℃ 二年 分子量： 399.39     化学名：  N-(2-Fluorophenyl)-3-oxo-5-(ethoxymethyl)-7-fluoro-1,2,3,5-tetrahydropyrido[1,2-a]benzimidazole-4-carboxamide 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。   生物活性 产品描述 一种GABA(A)receptor的部分激动剂，Ki值为0.2-2nM。 靶点 Ki:0.2-2nM (GABA(A)) 体外研究 RWJ-51204 binds to receptors in the cerebral cortex,cerebellum,or medulla-spinal cord with Ki ranging from 0.2 to 0.6nM. 体内研究 RWJ-51204 is orally active in anxiolytic efficacy tests.WJ 51204 dose-relatedly antagonizes PTZ-induced clonic convulsions when administered orally (ED50=0.04mg/kg).RWJ-51204 is effective in the conflict test in monkeys (ED50 of approximately 0.5mg/kg p.o.).RWJ-51204 potently impairs rotarod performance in rats (ED50=0.12mg/kg),and all rats given RWJ-51204 orally at 30mg/kg exhibit sedation,reduced skeletal muscle tone,and impairment of rotarod performance.   推荐实验方法(仅供参考) 激酶实验： For each sample,a portion of the membrane fraction containing 0.1 to 0.2mg of protein is incubated in 2mL of a 3mM phosphate-buffered solution containing 0.1 M NaCl and 0.01 to 0.03μCi of a 3H-labeled ligand [3H]Ro15-4513,[3H]flumazenil.The receptor-ligand binding reaction is allowed to reach equilibrium at an ambient temperature of 21-23℃ (30 min) and then the reaction is terminated by vacuum filtration to separate the incubation medium from the biological membranes.The membrane samples are washed to remove unbound ligand.The3H bound to each membrane sample is quantified using liquid scintillation spectrometry.   动物实验:   Adult rats are deprived of water for 48h and are deprived of food for at least 16h before testing.After the first 24h of water deprivation,they are placed in a sound-attenuating chamber for a training period,in which they are allowed 200 licks from a bottle containing tap water.The experiment is performed the next day.Vehicle or compounds are administered orally by gavage,and at specified times after dosing,rats are placed in the chamber and allowed access to tap water.The first lick at the stainless steel sipper tube of a water bottle initiates a 3-min test session in which every 20th lick is punished by a 0.2s,0.5mA shock (root mean square,measured across the electrodes) delivered via the sipper tube.If rats fail to drink within 5 min,the experiment is terminated,and they are evaluated for signs of CNS depression.Rats are not reused in this experiment.The anxiolytic effectiveness of a compound in this assay is determined from the number of rats,at each dose,that receive a number of shocks that is equal to or greater than the calculated 90th percentile of the number of shocks received by approximately 600 vehicle-treated rats.This criterion is eight shocks when rats are tested 1h after administration and 10 shocks when rats are tested 4h after administration.
保存条件：-20℃

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