Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LP-211 是一种可透过血脑屏障的选择性5-HT7受体激动剂,Ki 值为 0.58 nM,选择性高于 5-HT1A 受体和 D2受体,Ki 分别为188 和 142 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 283 | 现货 | ||
2 mg | ¥ 395 | 现货 | ||
5 mg | ¥ 652 | 现货 | ||
10 mg | ¥ 996 | 现货 | ||
25 mg | ¥ 1,950 | 现货 | ||
50 mg | ¥ 3,230 | 现货 | ||
100 mg | ¥ 4,790 | 现货 | ||
200 mg | ¥ 6,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 721 | 现货 |
产品描述 | LP-211 is a brain penetrant selective agonist for a 5-HT7 receptor (Ki: 0.58 nM), and >300-fold selectivity over the 5-HT1A receptor. |
靶点活性 | D2 receptor:142 nM (Ki), 5-HT1A receptor:188 nM (Ki), 5-HT7 receptor:0.58 nM (Ki) |
体外活性 | LP-211 showed high 5-HT 7 receptor affinity (Ki = 0.58 nM), high selectivity over 5-HT 1A and D 2 receptors (324- and 245-fold, respectively), and agonist properties (maximal effect = 82%, EC 50 = 0.60 microM) [1]. Pretreatment with LP-211 had no effect on Fos-like immunoreactivity but strongly increased the response produced by capsaicin [2]. |
体内活性 | After intraperitoneal injection in mice, LP-211 (10 mg/kg) rapidly reached the systemic circulation and entered the brain. Its brain concentration-time profile paralleled that in plasma [1]. SCI rats responded to LP-211 (0.003-0.3, mg/kg, i.v.) with dose-dependent increases in bladder capacity and residual volume [3]. LP-211 reduced synaptic integration in layer 5 pyramidal neurons, which was enhanced in neuropathic pain due to a dysfunction of dendritic hyperpolarization-activated-and-cyclic-nucleotide-regulated (HCN) channels [4]. |
激酶实验 | Human 5-HT1A serotonin receptors stably expressed in HEK293 cells were radiolabeled with 1.0 nM [3H]-8-OH-DPAT. Samples containing 40 μg of membrane protein and different concentrations of each compound ranging from 0.1 nM to 10 μM were incubated in a final volume of 500 μL of 50 mM Tris-HCl pH 7.4, 5 mM MgSO4 for 120 min at 37 °C. After this incubation time, samples were filtered through GF/C presoaked in polyethylenimine 0.5% for at least 30 min prior to use. The filters were washed twice with 1 mL of ice-cold buffer (50 mM Tris-HCl, pH 7.4). Nonspecific binding was determined in the presence of 10 μM 5-HT [1]. |
动物实验 | Mice were given the test compounds intraperitoneally (10 mg/kg) and were killed by decapitation at various times thereafter. Mixed arteriovenous trunk blood was collected in heparinized tubes, centrifuged at 3000g for 10 min, and the plasma was stored at -20 °C. Brain was removed immediately, blotted with paper to remove surface blood, and quickly frozen in dry ice. Compounds and their 1-arylpiperazine metabolites were extracted from plasma and brain homogenate and quantified by reversed-phase HPLC with UV detection (230 nm). Briefly: to 0.1 mL of plasma, 0.2 mL of 20 mM of ammonium bicarbonate and 0.02 mL of a methanolic solution of the internal standard (100 μg/mL) were added; samples were then extracted twice with 1.5 mL of hexane containing 1% of isoamyl alcohol, and the combined extracts were evaporated to dryness and reconstituted in 0.15 mL of the mobile phase, which was injected into the chromatographic column. Brain tissue was homogenized in distilled water (1 g/10 mL), and 1 mL of the homogenate was extracted twice with 1.5 mL of hexane/isoamyl alcohol as described for plasma. Then, the organic phase was shaken with 0.2 mL of the mobile phase (LP-211 only); after centrifugation, 0.1 mL of the aqueous phase was injected into the chromatographic column [1]. |
分子量 | 466.62 |
分子式 | C30H34N4O |
CAS No. | 1052147-86-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (192.87 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1431 mL | 10.7154 mL | 21.4307 mL | 53.5768 mL |
5 mM | 0.4286 mL | 2.1431 mL | 4.2861 mL | 10.7154 mL | |
10 mM | 0.2143 mL | 1.0715 mL | 2.1431 mL | 5.3577 mL | |
20 mM | 0.1072 mL | 0.5358 mL | 1.0715 mL | 2.6788 mL | |
50 mM | 0.0429 mL | 0.2143 mL | 0.4286 mL | 1.0715 mL | |
100 mM | 0.0214 mL | 0.1072 mL | 0.2143 mL | 0.5358 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
LP-211 1052147-86-0 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor Inhibitor LP211 Serotonin Receptor 5-hydroxytryptamine Receptor inhibit LP 211 inhibitor