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AUT1

AUT1

产品编号 T5183   CAS 1311136-84-1

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。

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AUT1 Chemical Structure
AUT1, CAS 1311136-84-1
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
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产品目录号及名称: AUT1 (T5183)
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纯度: 99.43%
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 250 mg/mL (732.36 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Rosato-Siri MD, et al. A Novel Modulator of Kv3 Potassium Channels Regulates the Firing of Parvalbumin-Positive Cortical Interneurons. J Pharmacol Exp Ther. 2015 Sep;354(3):251-60. 2. Brown MR, et al. Physiological modulators of Kv3.1 channels adjust firing patterns of auditory brain stem neurons. J Neurophysiol. 2016 Jul 1;116(1):106-21.
20(S)-Ginsenoside Rg3 2,2,2-Trichloroethanol Nigericin sodium salt SKF-96365 hydrochloride Linaprazan Miconazole XE991 Flupirtine maleate

相关化合物库

该产品包含在如下化合物库中:
膜蛋白靶向化合物库 已知活性化合物库 经典已知活性库 抗癌化合物库 离子通道库 NO PAINS 化合物库 钾通道分子库

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Keywords

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

 

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