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- 文献和实验
- 技术资料
- CAS号:
1311136-84-1
- 规格:
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg
| 规格: | 1mg | 产品价格: | ¥273.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥470.0 |
| 规格: | 5mg | 产品价格: | ¥629.0 |
| 规格: | 10mg | 产品价格: | ¥944.0 |
| 规格: | 25mg | 产品价格: | ¥1664.0 |
| 规格: | 50mg | 产品价格: | ¥2552.0 |
| 规格: | 100mg | 产品价格: | ¥3696.0 |
Product Introduction
Bioactivity
| 名称 | AUT1 |
| 描述 | AUT1 (AUT-1) is a novel specific modulator of Kv3 channels (EC50: 4.7 and 4.9 uM for Kv3.1b and Kv3.2a). |
| 细胞实验 | The population patch-clamp mode of an automated voltage clamp recording with IonWorks Quattro was used. Briefly, the effects on these channels were tested using 384-well population patch-clamp plates. Seal resistance was measured for each well, and cells were perforated by incubation with 100 mg/ml amphotericin B. Cells were held at 270 mV and stepped to 215 mV for 100 milliseconds (partial channel activation), and after 100 milliseconds at 270 mV, a second pulse to 140 mV was applied for 50 milliseconds (full channel activation). In all of the experiments, this voltage protocol was applied to cells before and following a 3-minute incubation with AUT1. 1-Cyclohexyl-1-[(7,8-dimethyl-2-oxo-1H-quinolin-3-yl)methyl]-3-phenylurea (10 mM), which we had previously found to be a potent and full activator of human Kv3.1 and Kv3.2 channels, was included in all assays as a standard. An external buffer with the addition of dimethyl sulfoxide (DMSO) was also tested to provide a vehicle baseline. Recordings were performed in the following buffers: Dulbecco's phosphate-buffered saline (PBS) with MgCl2 and CaCl2 as an extracellular solution and 50 mM KCl, 100 mM K-gluconate, 3.2 mM MgCl2, and 5 mM HEPES, pH 7.3 adjusted with KOH, as an intracellular solution. An online correction of 115–20 mV was applied to correct for junction potentials. The current signal was sampled at 10 kHz [1]. |
| 体外活性 | AUT1增强了人类重组Kv3.1b和Kv3.2a通道介导的电流。对于Kv3.1b和Kv3.2a,AUT1的pEC50值分别为5.33(4.7 μM)和5.31(4.9 μM)[1]。使用稳定表达大鼠Kv3.1通道的中国仓鼠卵巢细胞,较低浓度的AUT1可将Kv3.1电流的激活电压向负电位移动,从典型神经元静息电位引起的去极化所诱发的电流增加[2]。 |
| 存储条件 | Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (14.65 mM), Sonication is recommended. DMSO : 250 mg/mL (732.36 mM), Sonication is recommended. |
| 关键字 | schizophrenia | recombinant human Kv3 channels | PotassiumChannel | Potassium Channel | Kv3.2a channels | Kv3.2a | Kv3.1b channels | Kv3.1b | KcsA | Inhibitor | inhibit | human recombinant | dysfunction | corticolimbic circuits | AUT-1 | AUT1 | AUT 1 |
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| 相关库 | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Potassium Channel Targeted Library | NO PAINS Compound Library | Ion Channel Targeted Library | Multi-Target Compound Library | Pain-Related Compound Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
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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