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SSD114 hydrochloride  ≥98%

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包装规格：5mg 25mg in glass bottle
溶解性：溶于DMSO(130mg/ml超声)
产品描述：基本信息 产品编号： S10947  产品名称： SSD114 hydrochloride CAS: 2319790-02-6   储存条件 粉末 -20℃ 四年     分子式： C18H21ClF3N3O 溶于液体 -80℃ 6个月 分子量： 387.83 -20℃ 1个月 化学名：  SSD 114 HCl;SSD-114 HCl;SSD114 hydrochloride;SSD-114 hydrochloride;SSD 114 hydrochloride Solubility (25°C)：   体外:   DMSO   Ethanol 'mg/mL 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 2.5784mL 12.8922mL 25.7845mL 5mM 0.5157mL 2.5784mL 5.1569mL 10mM 0.2578mL 1.2892mL 2.5784mL   生物活性 产品描述 一种新型GABAB受体正变构调节剂。 靶点 GABAB receptor   体外研究 In the presence of 10µM GABA,SSD114 hydrochloride at 25µM significantly increases (to approximately 170% above basal levels) the [35S]GTPγS stimulation induced by GABA alone.SSD114 hydrochloride,added at 15 and 30µM,induces a leftward shift of the GABA concentration-response curve with a slight concomitant increase of maximal GABA stimulation at the highest concentration.In the presence of both 15 and 30µM SSD114 hydrochloride,the EC50 for GABA decreases by 2 and 2.5 fold,respectively,while the maximal stimulation (Emax) is potentiated only at the concentration of 30µM,reaching 161±5.09% over the basal value. 体内研究 The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F(5,30)=4.55,P<0.005].Post hoc analysis indicates that the onset of LORR is significantly lower in mouse groups pretreated with doses of SSD114 hydrochloride equal to or higher than 10mg/kg than in vehicle-treated mice.The duration of LORR is increased by pretreatment with SSD114 hydrochloride [F(5,30)=4.81,P<0.005].Post hoc analysis indicates that the duration of LORR is significantly longer in mouse groups pretreated with 10 and 100mg/kg SSD114 hydrochloride than in vehicle-treated mice.   推荐实验方法(仅供参考) 细胞实验:   Cells are transfected and seeded into 96-well microplates.24h after transfection,cells are washed twice with PBS and incubated in the presence or absence of SSD114 hydrochloride (different concentrations) for 15 min before substrate addition in a 96-well microplate.The Bioluminescence resonance energy transfer (BRET) ratio is calculated as the emission of YFP (530 to 570nm) over the emission of RLuc (370 to 470nm).The curves are fitted using Graph Pad Prism 5.0.The amplitude-weighted mean time constant is obtained by fitting the BRET recovery phase to a double exponential function.Δ BRET is calculated as the difference between the basal and the plateau of the BRET signal.   动物实验:   Male Sprague-Dawley rats and DBA mice,weighing 200 to 250 and 20 to 25g,respectively,are used.On the test day,mice are divided into six groups (n=6 each) matched by body weight.Mice are treated acutely and intraperitoneally with 0,1,3,10,30,and 100mg/kg SSD114 hydrochloride and sedation/hypnosis is measured.Specifically,after baclofen injection,each mouse is placed on its back once every 60 s until it is unable to right itself within 60 s.The time between baclofen injection and the start of the 60-s interval during which the mouse is unable to right itself is measured as the onset of loss of righting reflex (LORR).Each mouse is then left undisturbed on its back until it spontaneously regained its righting reflex (determined as having at least three paws under its body).Complete recovery of the righting reflex is defined as the mouse being able to turn itself upright twice more within 60 s.If this criterion is not fulfilled,the mouse is left undisturbed until it spontaneously regained its righting reflex.The time between loss and recovery of righting reflex is monitored in each mouse and defined as the duration of LORR. Observations are conducted by an operator unaware of the drug treatment.
保存条件：-20℃

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