Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NS3861 是烟碱型乙酰胆碱受体的激动剂,对α3β4 nAChR 具有高亲和力。能够分别与α3β4 (Ki:0.62 nM)、α3β2 (Ki:25 nM)、α4β4 (Ki:7.8 nM)、α4β2 (Ki:55 nM) 结合。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 178 | 现货 | ||
5 mg | ¥ 383 | 现货 | ||
10 mg | ¥ 713 | 现货 | ||
25 mg | ¥ 1,690 | 现货 | ||
50 mg | ¥ 2,860 | 现货 | ||
100 mg | ¥ 4,230 | 现货 | ||
500 mg | ¥ 9,180 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 397 | 现货 |
产品描述 | NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and bind with high affinity to heteromeric α3β4 and α4β2 nAChRs. NS3861 displays the β-subunit preference and a complete lack of activation at α4-containing receptors. The maximal efficacy of NS3861 appeared solely dependent on the nature of the ligand-binding domain. Furthermore, a principal subunit serine to threonine substitution may explain the lack of NS3861 activation at α4-containing receptors. |
靶点活性 | α3β4:1 μm(Ki), α4β4 (1:4):1.9 μm(Ki), α4β4 (4:1):1.2 μm(Ki), α3β2:1.6 μm(Ki) |
体外活性 | NS3861 was found to activate wild-type α3β4 nAChRs (Figs. 3R and 4) but did not activate wild-type α4β2. Whereas NS3861 was a partial agonist at α3β4, it proved to be a full agonist at α3β2 albeit with ~10-fold lower potency consistent with the binding affinities. Efficacy at the α3/α4 + β4/β2 receptor was almost identical to that of wild-type α3β4, whereas no efficacy could be seen at α4/α3 + β2/β4[1]. |
分子量 | 284.22 |
分子式 | C12H14BrNS |
CAS No. | 216853-59-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (351.84 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.5184 mL | 17.592 mL | 35.184 mL | 87.96 mL |
5 mM | 0.7037 mL | 3.5184 mL | 7.0368 mL | 17.592 mL | |
10 mM | 0.3518 mL | 1.7592 mL | 3.5184 mL | 8.796 mL | |
20 mM | 0.1759 mL | 0.8796 mL | 1.7592 mL | 4.398 mL | |
50 mM | 0.0704 mL | 0.3518 mL | 0.7037 mL | 1.7592 mL | |
100 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8796 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。
NS3861 216853-59-7 Neuroscience AChR α3β4 nAChR inhibit Inhibitor Heteromeric Patch Clamp Nicotinic acetylcholine receptors nAChR Pharmacology NS-3861 NS 3861 inhibitor