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- CAS号：
550999-75-2
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mg | 产品价格： | ￥274.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥532.0 |
| 规格： | 5mg | 产品价格： | ￥628.0 |
| 规格： | 10mg | 产品价格： | ￥808.0 |
| 规格： | 25mg | 产品价格： | ￥1344.0 |
| 规格： | 50mg | 产品价格： | ￥1928.0 |
| 规格： | 100mg | 产品价格： | ￥2624.0 |
Product Introduction
Bioactivity
| 名称 | Encenicline |
| 描述 | Encenicline (EVP-6124) is a selective α7 nicotinic acetylcholine receptor (nAChRs) agonist in development for treating cognitive impairment in schizophrenia and Alzheimer's disease. |
| 细胞实验 | Experiments were carried out with human a7 nAChRs expressed in Xenopus laevis oocytes.?Oocytes were prepared, injected with cDNA encoding a7 nAChR subunits, and recorded using standard procedures.?Additional studies were carried out with rat a3b4, a4b2, and muscle a1b1gd nAChRs expressed in oocytes.?Briefly, ovaries were harvested from X. laevis females that were deeply anesthetized by cooling at 4℃ and with tricaine mesylate (3-aminobenzoic acid ethyl ester, methane sulfonate salt, 150 mg/l).?Small pieces of ovary were isolated in sterile Barth solution (88 mM NaCl, 1 mM KCl, 2.4 mM NaHCO3, 10 mM HEPES, 0.82 mM MgSO4·7H2O, 0.33 mM Ca(NO3)2·4H2O, and 0.41 mM CaCl2·6H2O, pH 7.4) and supplemented with 20 mg/ml kanamycin, 100 μg/ml penicillin, and 100 mg/ml streptomycin.?Injections of cDNAs encoding for the receptors were performed in at least one hundred oocytes using an automated ?injection device;?and receptor expression was examined at least two days later.?Oocytes were impaled with two electrodes filled with 3 M KCl, and their membrane potentials were ?maintained at ?80 mV throughout the experiment.?All recordings were performed ?at 18 C and cells were superfused with OR2 medium (82.5 mM NaCl, 2.5 mM KCl, 5 mM HEPES, 1.8 mM CaCl2·2H2O, and 1 mM MgCl2·6H2O, pH 7.4).?Currents were recorded using an automated process equipped with standard two-electrode voltage-clamp configuration.Data were captured and analyzed using Matlab or Excel software.ACh and EVP-6124 were prepared as concentrated stock solutions in water and then diluted in the recording medium to obtain the desired test concentrations.?All experiments were carried out using three or more cells[1]. |
| 动物实验 | For the experiments using natural forgetting (a 24 h retention interval) and MLA, twenty-four 2-month-old male Wistar rats .?In the doseeresponse experiment, the rats were 2.5 months old (average body weight: 319 g). For the coadministration of EVP-6124 and MLA , the rats were 3 months old (average body weight: 357 g). For the co-administration of EVP-6124 and MLA, the rats were 4 months old (average body weight: 407 g). Across the 3 experiments, rats were tested a total of 5e10 times.?The effects of EVP-6124 on memory consolidation in particular were investigated in the natural forgetting test in the ORT, using twentyfour 3-month-old Wistar rats (average body weight: 357 g). All 24 rats received each treatment, i.e. each rat was tested 7 times in two experiments.?All animals were housed individually, which improves ORT performance, in standard type III Makrolon cages on sawdust bedding.?The animals were on a reversed 12/12-h light/dark cycle (lights on from 19:00 to 7:00 h);?and food and water were given ad libitum.?The rats were housed and tested in the same room.?A radio, playing softly provided background noise to mask noises in the room.?All testing was performed between 9:00 and 18:00 h under low illumination (20 lux)[1]. |
| 体外活性 | In co-application experiments of EVP-6124 with acetylcholine, sustained exposure to EVP-6124 in functional investigations in oocytes caused desensitization at concentrations greater than 3 nM, while lower concentrations (0.3-1 nM) caused an increase in the acetylcholine-evoked response.?These actions were interpreted as representing a co-agonist activity of EVP-6124 with acetylcholine on α7 nAChRs.?The concentrations of EVP-6124 that resulted in physiological potentiation were consistent with the free drug concentrations in brain that improved memory performance in the ORT[2]. |
| 体内活性 | EVP-6124 showed selectivity for α7 nAChRs and did not activate or inhibit heteromeric α4β2 nAChRs.?EVP-6124 had good brain penetration and an adequate exposure time.?EVP-6124 (0.3 mg/kg) significantly restored memory function in scopolamine-treated rats (0.1 mg/kg) in an object recognition task (ORT).?Although donepezil at 0.1 mg/kg, p.o. or EVP-6124 at 0.03 mg/kg, p.o. did not improve memory in this task, co-administration of these sub-efficacious doses fully restored memory.?In a natural forgetting test, an ORT with a 24 h retention time, EVP-6124 improved memory at 0.3 mg/kg, This improvement was blocked by the selective α7 nAChR antagonist methyllycaconitine (0.3 mg/kg or 10 μg)[1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 60 mg/mL (187.01 mM), Sonication is recommended. |
| 关键字 | Nicotinic acetylcholine receptors | nAChR | Inhibitor | inhibit | EVP6124 | EVP 6124 | Encenicline |
| 相关产品 | Mitotane | Hexamethonium Bromide | Ethyl (triphenylphosphoranylidene) acetate | Urethane | Levamisole hydrochloride | Arecoline | Choline chloride | Adenine | N,N-Dicyclohexylcarbodiimide | Propoxur | Adiphenine hydrochloride | Ribavirin |
| 相关库 | Bioactive Compound Library | Bioactive Compounds Library Max | ReFRAME Related Library | Anti-Alzheimer's Disease Compound Library | Neurotransmitter Receptor Compound Library | Neuronal Signaling Compound Library | NO PAINS Compound Library | Ion Channel Targeted Library | Membrane Protein-targeted Compound Library | Anti-Neurodegenerative Disease Compound Library | Pain-Related Compound Library | Human Metabolite Library |
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体系，可与质子结合，故其碱性（PKb=8.8）较吡咯(pKb=13.6)强，也比苯胺（pKb=9.3）强，能与强酸作用生成较稳定的盐。但比氨(pKb=4.75)弱，也比脂肪叔胺（三甲胺的pKb=4.22）弱。原因在于吡啶环上未参与共轭体系的这一对未共用电子对处于sp2杂化轨道上，其s成分较sp3杂化轨道多，受原子核束缚强，因而较难与H+结合。 吡啶与水能以任意比例混溶，同时又能溶解大多数极性及非极性有机化合物，它是一个良好的溶剂。吡啶具有高水溶性的原因，除分子极性外，是由于其氮原子上一对未参与环
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 Encenicline【550999-75-2】
￥274 - 2624
