ZSET1446  ≥98%

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包装规格:5mg 25mg 100mg in glass bottle
溶解性:溶于DMSO(≥34mg/ml)
产品描述:基本信息 产品编号: Z10072 产品名称: ZSET1446 CAS: 887603-94-3   储存条件 粉末 -20℃ 四年     分子式: C15H12N2O 溶于液体 -80℃ 6个月 分子量: 236.27 -20℃ 1个月 化学名:  1 inverted exclamation mark ,3 inverted exclamation mark -Dihydro-2H-spiro[imidazo[1,2-a]pyridine-3,2 inverted exclamation mark -inden]-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。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 4.2324mL 21.1622mL 42.3245mL 5mM 0.8465mL 4.2324mL 8.4649mL 10mM 0.4232mL 2.1162mL 4.2324mL   生物活性 产品描述 一种新的促进认知药,在不同的阿尔茨海默病模型中,能够改善学习功能障碍。 靶点 Calcium Channel nAChR   体外研究 ZSET1446 (100pM-10nM) exerts limited effects on the basal neuronal excitability and synaptic transmission.ZSET1446 potentiates the facilitatory effect of nAChR stimulation on sPSC frequency.ZSET1446 potentiates the increase in sIPSC frequency by local application of nicotine (5µM;2minutes) without affecting the basal sIPSC frequency at the range of 10pM to 1nM. 体内研究 ZSET1446 enhances object recognition memory in mice and ameliorates cognitive impairment caused by scopolamine in rats.Concomitant administration of subeffective doses of ZSET1446 and memantine significantly ameliorates the cognitive performance in the novel object recognition task in both mice and rats.Moreover,oral administration of ZSET1446 or memantine increases the extracellular level of ACh in the hippocampus as compared with the control.Further,concomitant administration of subeffective doses of ZSET1446 and memantine significantly increases the extracellular level of ACh as compared with the group of ZSET1446 or memantine alone.ZSET1446 (0.002,0.01,and 0.1mg/kg,p.o.) ameliorates cognitive deficits of SAMP8 after 4,8,12,and 16 weeks of treatment in a novel object recognition test.ZSET1446 also reduces grading scores of SAMP8 after 16 weeks of treatment.Further,8-week treatment of ZSET1446 significantly reduces the total number of Aβ-positive granules in the hippocampus.   推荐实验方法(仅供参考) 动物实验:   The experimental apparatus consists of a Plexiglas open-field box [25 cm (width)×41cm (length)×17 cm (depth),model TP-105],the floor of which is covered with sawdust.The apparatus is located in a sound-attenuated room.The procedure for the novel object recognition task consists of three different sessions:habituation,training,and retention sessions.Each mouse is individually habituated to the box,with 10 min of exploration in the absence of objects (day 1:habituation session).ZSET1446 at doses of 0.001,0.003,0.01,and 0.03mg/kg and/or memantine at doses of 3 and 10mg/kg is orally administered 60 min before the training trial.In the experiment of injection of nicotinic receptor antagonists,oral administration of ZSET1446 and i.p.injection of mechamylamine or DHbE at each dose of 1mg/kg are given 60 min before the training trial.During the training session,two different novel objects are symmetrically fixed to the floor in the box,and each animal is allowed to explore in the box for 10 min (day 2:training session).These objects are different in shape and color but similar in size.The mice are considered to be exploring the object when the mouse is facing,touching, or sniffing the object.The time spent for exploring each object is manuallymeasured by a stopwatch.In the training session, locomotor activity is simultaneously measured for a period of 10 min automatically,using an Animex Auto placed under the open-field box.After the training trial, mice are immediately returned to their home cages.
保存条件:-20℃