NS3861
目录号: PL07676 纯度: ≥99%
CAS No. :216853-59-7
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中文名称
NS3861
英文名称
NS3861
英文别名
NS3861
Cas No.
216853-59-7
分子式
C12H14BrNS
分子量
284.22
包装储存
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
NS3861 是烟碱型乙酰胆碱受体 (nAChRs) 的激动剂,对 α3β4 nAChR 具有高亲和力。与α3β4、α3β2、α4β4、α4β2 的结合 Ki 值分别为 0.62、25、7.8、55 nM。
生物活性
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding K i values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.
性状
Solid
体外研究(In Vitro)
NS3861 displays the opposite β-subunit preference and a complete lack of activation at α4-containing receptors in HEK293 cell lines. NS3861 selectively activates α3- but not α4-containing nAChRs and it displays higher efficacy at the α3β2 receptor compared with the α3β4 receptor, with EC50s of 1.7 and 0.15 μM for α3β2 and α3β4 receptor, respectively.
NS3861 shows high affinity and partial agonist properties in α3β4-expressed nAChRs. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
NS3861 enhances fecal pellet expulsion in a dose-dependent manner in mice that received long-term, but not short-term, morphine treatment. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Kasper Harps?e, et al. Molecular determinants of subtype-selective efficacies of cytisine and the novel compound NS3861 at heteromeric nicotinic acetylcholine receptors. J Biol Chem. 2013 Jan 25;288(4):2559-70.
[2]. Aravind R Gade, et al. Enhanced Sensitivity of α3β4 Nicotinic Receptors in Enteric Neurons after Long-Term Morphine: Implication for Opioid-Induced Constipation. J Pharmacol Exp Ther. 2016 Jun;357(3):520-8.
溶解度数据
In Vitro: DMSO : 100 mg/mL (351.84 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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