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Eptapirone  ≥98%

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包装规格：25mg in glass bottle
溶解性：溶于DMSO（50mg/mL 超声）
产品描述：基本信息 产品编号： E10406 产品名称： Eptapirone CAS: 179756-58-2   储存条件 粉末 -20℃ 四年     分子式： C16H23N7O2 溶于液体 -80℃ 两年 分子量 345.40 -20℃ 1个月 化学名：  4-methyl-2-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]-1,2,4-triazine-3,5-dione Solubility (25°C)：   体外:   DMSO 69 mg/mL (199.76mM) Ethanol 39 mg/mL (112.91mM) Water Insoluble 体内(现配现用): 请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5 mg/mL (7.24mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (7.24mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50μL Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline)  Solubility: ≥ 2.5 mg/mL (7.24mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (7.24mM，饱和度未知) 的澄清溶液。以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均 匀。 请依序添加每种溶剂：10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (7.24mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (7.24mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例，取 100μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中，混合均匀。 ＜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 2.8952mL 14.4760mL 28.9519mL 5mM 0.5790mL 2.8952mL 5.7904mL 10mM 0.2895mL 1.4476mL 2.8952mL 50mM 0.0579mL 0.2895mL 0.5790mL   生物活性 产品描述 一种强效，选择性，疗效高的 5HT1A 受体激动剂, 有显著的抗焦虑和抗抑郁潜力。 靶点 5-HT1A Receptor   体外研究 The affinity of Eptapirone (F11440) for 5-HT1Abinding sites (pKi, 8.33) was higher than that of buspirone (pKi , 7.50), and somewhat lower than that of flesinoxan (pKi , 8.91).In vivo, Eptapirone (F11440) was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively). Eptapirone (F11440), shown here to be a potent, selective, high efficacy 5-HT1Areceptor agonist, appears to have the potential to exert marked anxiolytic and antidepressant activity in humans.   推荐实验方法(仅供参考) Cell Assay Eptapirone (F11440) is dissolved in DMSO. The HeLa cell line permanently transfected with the human 5-HT1A receptor gene and permanently expressing the 5-HT1A receptor protein (HA7). In subsequent experiments, the maximum effect of Eptapirone (F11440) is compared with those of other compounds by repeated testing (n=9) at a concentration of 10-5 M (i.e., a concentration at which the reference compounds used here appeared to attain their maximal effects) in a first series of experiments and at 10-4 M in a second series. Data from each series were analyzed statistically by means of a one-way analysis of variance followed by sequential paired comparisons by means of Newman-Keuls tests.   Animal Administration Rats For in vivo studies, F 11440 was suspended in distilled water by adding Tween 80 (2 drops/10 ml). When injected i.v., F 11440 was dissolved in a mixture of 60% PEG and 40% physiological saline. Doses are expressed as the weight of the free base. Twenty-four hours before use in the experiments, rats were housed individually in a restricted area (accessible only to the experimenter) and received 15 g standard laboratory food (water continued to be available freely). Experiments, consisting of drug treatments after which animals were decapitated and trunk blood was collected, were conducted between 8:00 a.m. and 10:30 a.m. F 11440 (or vehicle) was administered 60 min before decapitation when given p.o., and 30 min before decapitation when given i.p..
保存条件：-20℃

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