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LP-211  ≥98%

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包装规格：100mg in glass bottle
溶解性：溶于乙醇（50mg/mL 超声），溶于DMSO（100mg/mL 超声）
产品描述：基本信息 产品编号： L10396 产品名称： LP-211 CAS: 1052147-86-0   储存条件 粉末 -20℃ 四年     分子式： C30H34N4O 溶于液体 -80℃ 六个月 分子量 466.62 -20℃ 一个月 化学名：  N-[(4-cyanophenyl)methyl]-6-[4-(2-phenylphenyl)piperazin-1-yl]hexanamide Solubility (25°C)：   体外:   DMSO 100 mg/mL (214.31mM; Need ultrasonic) Ethanol 50 mg/mL (107.15mM; Need ultrasonic) Water   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 (5.36mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (5.36mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0mg/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 50 μ L 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 (5.36mM); Clear solution 此⽅案可获得 ≥ 2.5 mg/mL (5.36mM，饱和度未知) 的澄清溶液。 以 1 mL 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 (5.36mM); Clear solution 此⽅案可获得 ≥ 2.5mg/mL (5.36mM，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 25.0mg/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 2.1431mL 10.7154mL 21.4307mL 5mM 0.4286mL 2.1431mL 4.2861mL 10mM 0.2143mL 1.0715mL 2.1431mL   生物活性 产品描述 一种选择性的，可透过血脑屏障的 5-HT7 受体激动剂，Ki 值为 0.58nM，选择性高于 5-HT1A 受体 (Ki，188nM) 和 D2 受体 (Ki，142nM)。 靶点 HT7 Receptor 0.58nM (Ki) HT1A Receptor 188nM (Ki) D2 Receptor 142nM (Ki) 体外研究 LP-211 is a selective 5-HT7 receptor agonist, with a Ki of 0.58nM, 324- and 245-fold selectivity over 5-HT1A receptor (Ki, 188nM) and D2 receptor (Ki, 142nM). LP-211 shows agonist properties with an EC50 of 0.6μM. 体内研究 LP-211 (10 mg/kg, i.p.) rapidly reaches the systemic circulation in the mouse, with mean Cmax of 0.76 ± 0.32μg/mL at 30 min. LP-211 (0.003-0.3 mg/kg, i.p.) significantly increases the micturition volume in a dose-dependent manner, and causes significant increases in voiding efficiency in spinal cord-injured (SCI) rats, and such effects can be completely reversed by SB269970. LP-211 (0.25 and 0.50 mg/kg i.p.) improves consolidation of chamber-shape memory in rats, resulting in significant novelty-induced hyperactivity and recognition.   推荐实验方法(仅供参考) Kinase Assay Binding of [3H]-LSD at rat cloned 5-HT7 receptor is performed in the assay. In 1mL of incubation buffer (50mM Tris, 10mM MgCl2 and 0.5mM EDTA, pH 7.4) are suspended 30μg of membranes, 2.5nM [3H]-LSD, LP-211 (6−9 concentrations). The samples are incubated for 60 min at 37°C. The incubation is stopped by rapid filtration on GF/A glass fiber filters (presoaked in 0.5% polyethylenimine for 30 min). The filters are washed with 3 × 53mL of ice-cold buffer (50mM Tris, pH 7.4). Nonspecific binding is determined in the presence of 10μM 5-CT. Approximately 90% of specific binding is determined under these conditions   Animal Administration RatsThirty male adult Wistar rats (300-450 g) are assessed for novelty preference behavior after acute treatment (administered immediately after the training session and 24 h before the test session). After a 4 weeks' wash out, the rPDT is conducted to evaluate attraction from a greater/uncertain reward, with a sub-chronic treatment (five injections, immediately after sessions which follow the indifferent point). Food restriction, imposed by the experimenter through a limited quantity of food given at the end of each rPDT session, is applied to increase motivation to work for food delivery. All behavioral tests take place between 9:30 am and 4:00 pm. Rats are randomly assigned to treatment (LP-211 at 0.25 or 0.50 mg/kg i.p.) and control groups (injection volume 10mL/kg; n = 10 per group). The brain penetrant 5-HT7R agonist LP-211 is dissolved in a vehicle solution of 1% dimethyl sulfoxide (DMSO) in saline (0.9%NaCl). Control group receives the vehicle strictly in the same conditions.
保存条件：-20℃

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