Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AUT1 是 Kv3 钾离子通道调节剂,对人重组 Kv3.1b 和 Kv3.2a 的pEC50值分别为 5.33 和 5.31,对其活性是对人重组 Kv3.3 通道的 10 倍,pEC50值为 4.5。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 395 | 现货 | ||
5 mg | ¥ 957 | 现货 | ||
10 mg | ¥ 1,450 | 现货 | ||
25 mg | ¥ 2,590 | 现货 | ||
50 mg | ¥ 3,880 | 现货 | ||
100 mg | ¥ 5,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,090 | 现货 |
产品描述 | AUT1 (AUT-1) is a novel specific modulator of Kv3 channels (EC50: 4.7 and 4.9 uM for Kv3.1b and Kv3.2a). |
靶点活性 | Kv3.2a:4.9 μM, Kv3.1b:4.7 μM |
体外活性 | AUT1 increased the current mediated by human recombinant Kv3.1b and Kv3.2a channels. pEC50 values for AUT1 were 5.33 (4.7 μM) and 5.31 (4.9 μM) for Kv3.1b and Kv3.2a, respectively [1]. Using Chinese hamster ovary cells stably expressing rat Kv3.1 channels, lower concentrations of AUT1 shift the voltage of activation of Kv3.1 currents toward negative potentials, increasing currents evoked by depolarization from typical neuronal resting potentials [2]. |
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]. |
分子量 | 341.36 |
分子式 | C18H19N3O4 |
CAS No. | 1311136-84-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (732.36 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.9295 mL | 14.6473 mL | 29.2946 mL | 73.2365 mL |
5 mM | 0.5859 mL | 2.9295 mL | 5.8589 mL | 14.6473 mL | |
10 mM | 0.2929 mL | 1.4647 mL | 2.9295 mL | 7.3236 mL | |
20 mM | 0.1465 mL | 0.7324 mL | 1.4647 mL | 3.6618 mL | |
50 mM | 0.0586 mL | 0.2929 mL | 0.5859 mL | 1.4647 mL | |
100 mM | 0.0293 mL | 0.1465 mL | 0.2929 mL | 0.7324 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。
AUT1 1311136-84-1 Membrane transporter/Ion channel Potassium Channel Kv3.1b corticolimbic circuits inhibit dysfunction recombinant human Kv3 channels human recombinant KcsA schizophrenia AUT 1 AUT-1 Inhibitor Kv3.2a inhibitor