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SX-3228  

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包装规格：5mg in glass bottle
产品描述：基本信息 产品编号： S10951 产品名称： SX-3228 CAS: 156364-04-4   储存条件 粉末 -20℃ 四年 分子式： C18H18N4O3 溶于液体 -80℃ 二年 分子量： 338.36     化学名：  6-BENZYL-3-(5-METHOXY-1,3,4-OXADIAZOL-2-YL)-1,5,7,8-TETRAHYDRO-1,6-NAPHTHYRIDIN-2-ONE 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 一种选择性苯二氮卓类(benzodiazepine1，BZ1)受体激动剂 靶点 IC50:17nM (BZ1 receptor)   体外研究 SX-3228 is a selective ligand for the BZ1 receptor.Among the BZ-receptor subtypes,SX-3228 preferentially binds to the BZ1 receptor (IC50=17nM).It has very weak affinity for the BZ2 receptor (spinal cord: IC50=127nM),and virtually no affinity for the peripheral type BZ receptor (kidney:IC50>10000nM).A compound with similar selectivity,SX-3228 has been shown to bind to BZ receptors,but not to dopamine (D1,D2),serotonin (5-HT1,5-HT2 and 5-HT3 subtypes),noradrenaline (α1,α2,β),GABA or acetylcholine (muscarinic) subtypes. 体内研究 Administration of 0.5-2.5mg/kg SX-3228 to rats during the light phase induces a significant reduction of rapid-eyemovement sleep (REMS) (P<0.05) during the third recording hour.Administration of SX-3228 (0.5-2.5mg/kg) at the beginning of the dark period significantly and dose-dependently reduces waking (W) and increases slow wave sleep (SWS) during the 6-h recording period (P<0.05-0.01);however,significant changes during the last recording hour are restricted to the 2.5mg/kg dose (P<0.01).   推荐实验方法(仅供参考) 动物实验:   Rats Twelve male Wistar rats (350-380g) are used.Subcutaneous (sc) injections are given in a final volume of 1.0mL/kg.All rats are given the corresponding volume of control solution (saline+Tween-80) in the control sessions. Following sc injection,a 6-h sleep recording is started at approximately 8:00 a.m.At least 4 days are allowed to elapse between injections to avoid long-lasting and rebound effects on sleep.The effects of SX-3228 0.5-2.5mg/kg are studied in one group of animals (N=6) during the light phase of the 12-h light:12-h dark cycle,starting 1h after the beginning of the light period.Polysomnographic recordings are started immediately after control solution or drug administration. Each rat receives all four treatments (control,and 0.5,1.0,2.5mg/kg SX-3228).
保存条件：-20℃

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