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U-101017  

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包装规格：1mg in glass bottle
产品描述：基本信息 产品编号： U10103 产品名称： U-101017 CAS: 170568-47-5   储存条件 粉末 -20℃ 四年 分子式： C23H27ClN4O3 溶于液体 -80℃ 一年 分子量： 442.94     化学名：  Imidazo(1,5-a)quinoline-3-carboxylic acid,7-chloro-5-(((3R,5S)-3,5-dimethyl-1-piperazinyl)carbonyl)-,1,1-dimethylethyl ester,rel- 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benzodiazepine受体和GABAA受体的部分激动剂，具有抗焦虑的作用。 靶点 GABA Receptor   体外研究 PNU-101017 potentiates GABA-stimulated Cl-currents at low concentrations (<1μM).U-101017 concentrationdependently inhibits the binding of [3H]FNZ to the membrane preparation of rat cerebral cortex in vitro with Ki of 3.37±0.22nM. 体内研究 Pre-ischemic treatment with either PNU-101017 significantly protects the CA1 neuronal population,and PNU-101017 reduces the loss to 50%.Delaying PNU-101017 administration until immediately after reperfusion does not reduce the neuroprotective activity.U-101017 (30μmol/kg,p.o.) time-dependently blocks [3H]FNZ binding to the mouse cerebral cortex.U-101017 dose-dependently decreases the levels of cGMP with ED50s of 260.0 (163-425) and 0.37 (0.12-1.04) in nonstressed and foot shock-stressed mice,respectively.Flumazenil,an antagonist of GABAA receptors,has no significant effect on cGMP in nonstressed mice,but pretreatment with flumazenil significantly blocks U-101017 (10μmol/kg,p.o.)-induced reductions in cGMP.In stressed mice,flumazenil is ineffective in altering cerebellar cGMP,but pretreatment with these doses of flumazenil significantly (p<0.01) blocks U-101017-induced attenuation of stress-induced elevations in cGMP.   推荐实验方法(仅供参考) 动物实验:   Three groups of gerbils (N=9-11/group) are treated i.p.with either vehicle (0.05 N HCl),PNU-101017 (30mg/kg) or diazepam (10mg/kg) 30 min prior to ischemia and again 2h after reperfusion.Two other groups receive PNU-101017 or diazepam immediately after reperfusion and again 2h later.The tested doses of PNU-101017 and diazepam are selected from past studies demonstrating their neuroprotective efficacy in the gerbil forebrain ischemia model.The administration of the second dose at 2h after reperfusion is consistent with previous dosing with other effective compounds tested in the gerbil.The 0.05 N HCl vehicle has been employed for i.p.dosing with other test compounds and is devoid of toxicity or acute distress production.
保存条件：-20℃

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