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首页 / 抑制剂/激动剂 / 神经信号通路 / AChR / Xanomeline/诺美林

Xanomeline/诺美林 {[allProObj[0].p_purity_real_show]}

货号：A114713 同义名： LY-246708

Xanomeline is a functionally selective M1/M4 agonist, used in the study of both Alzheimer's disease and schizophrenia.

Xanomeline/诺美林 化学结构 CAS号：131986-45-3
Xanomeline/诺美林 化学结构
CAS号：131986-45-3
Xanomeline/诺美林 3D分子结构
CAS号：131986-45-3
Xanomeline/诺美林 化学结构 CAS号：131986-45-3
Xanomeline/诺美林 3D分子结构 CAS号：131986-45-3
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Xanomeline/诺美林 纯度/质量文件 产品仅供科研

货号：A114713 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 AChE ↓ AChR ↓ mAChR ↓ nAChR ↓ 其他靶点 纯度
Donepezil +++

bAChE, IC50: 8.12 nM

hAChE, IC50: 11.6 nM

 		98%
Loganin ++

AChE, IC50: 3.95 μM

 		99%+
topride HCl ++

AChE, IC50: 2.04 μM

 		98%
Dehydroevodiamine HCl ✔ 99%+
Jatrorrhizine ++

AChE, IC50: 872 nM

 		99%+
Palmatine ++

AChE, IC50: 0.51 μM

 		95%
(-)-Huperzine A ++++

AChE (G4 form), Ki: 7 nM

 		98%
Galanthamine HBr ++

AChE, IC50: 0.35 μM

 		98%
Trospium chloride ✔ 99%
Tiotropium Bromide Monohydrate ✔ 97%
Gallamine Triethiodide +

AChR, IC50: 68.0 μM

 		98%
Hexamethonium Bromide ✔ 99%
Pancuronium dibromide ✔ 98%
Neostigmine bromide ✔ 98%
Orphenadrine citrate ✔ 98%
Oxybutynin ✔ 98%
Irsogladine ✔ PDE 99%
Pyridostigmine bromide ✔ 99+%
Rivastigmine +

AChR, IC50: 5.5 μM

 		98%
Paroxetine HCl ✔ 99%
Rocuronium Bromide ✔ 98%
Tropicamide +++

M4 mAChR, IC50: 8 nM

 		98%
Diphenmanil methylsulfate ✔ 99%
Umeclidinium bromide ✔ 95%
Otilonium bromide ✔ 98%
Flavoxate HCl +

mAChR, IC50: 12.2 μM

 		99%
Ipratropium bromide ✔ 98%
Diphenidol HCl ✔ 98%
Darifenacin hydrobromide ++++

M3 mAChR, pKi: 8.9

 		98%
Aclidinium Bromide ++++

M2 mAChR, Ki: 0.1 nM

M4 mAChR, Ki: 0.21 nM

 		98%
Oxybutynin chloride ✔ 99%
Pentoxyverine citrate ✔ 98%
Solifenacin ✔ 98%
Catharanthine ✔ 98%
Benzethonium chloride +++

α4β2 nAChRs, IC50: 49 nM

α7 nAChRs, IC50: 122 nM

 		99+%
Vinblastine sulfate +

nAChR, IC50: 8.9 μM

 		99%
PNU-120596 ++

α7 nAChR, EC50: 216 nM

 		99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Xanomeline/诺美林 生物活性

描述 Xanomeline is a subtype selective muscarinic M 1 receptor agonist and a potential new treatment for Alzheimer's disease. Intraperitoneal administration of xanomeline significantly suppressed serum and splenic TNF levels, alleviated sickness behavior, and increased survival during lethal murine endotoxemia[3]. Moreover, xanomeline is a potent agonist at 5-HT1A and 5-HT1B receptors and an antagonist at 5-HT2 receptor subtypes. Xanomeline induced an increase in cytoplasmic Ca2+ concentration in SH-SY5Y cells expressing recombinant human 5-HT2C receptors[4].

Xanomeline/诺美林 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03697252 Schizophrenia Phase 2 Recruiting November 5, 2019 United States, Arkansas ... 展开 >> Woodland International Research Group, LLC Recruiting Little Rock, Arkansas, United States, 72211 United States, California Synergy East Recruiting Lemon Grove, California, United States, 91945 Collaborative Neuroscience Network, LLC. Recruiting Long Beach, California, United States, 90806 NRC Research Institute Recruiting Orange, California, United States, 92868 Artemis Institute for Clinical Research Recruiting San Diego, California, United States, 92103 United States, Georgia Atlanta Center for Medical Research Recruiting Atlanta, Georgia, United States, 30331 United States, Maryland CBH Health, LLC Recruiting Gaithersburg, Maryland, United States, 20877 United States, New Jersey Hassman Research Institute Recruiting Berlin, New Jersey, United States, 08009 United States, Ohio Midwest Clinical Research Center (and IP Shipment) Recruiting Dayton, Ohio, United States, 45417 United States, Texas Community Clinical Research, Inc. Recruiting Austin, Texas, United States, 78754 InSite Clinical Research, LLC Recruiting DeSoto, Texas, United States, 75115 Pillar Clinical Research, LLC Recruiting Richardson, Texas, United States, 75080 收起 <<
NCT02831231 Schizophrenia Phase 1 Completed - United States, Ohio ... 展开 >> Medpace Cincinnati, Ohio, United States, 45227 收起 <<

Xanomeline/诺美林 参考文献

[1]van Harten PN, Tenback DE. Tardive dyskinesia: clinical presentation and treatment. Int Rev Neurobiol. 2011;98:187-210.

[2]Si W, Zhang X, et al. A novel derivative of xanomeline improves fear cognition in aged mice. Neurosci Lett. 2010 Apr 5;473(2):115-9.

[3]Rosas-Ballina M, Valdés-Ferrer SI, Dancho ME, Ochani M, Katz D, Cheng KF, Olofsson PS, Chavan SS, Al-Abed Y, Tracey KJ, Pavlov VA. Xanomeline suppresses excessive pro-inflammatory cytokine responses through neural signal-mediated pathways and improves survival in lethal inflammation. Brain Behav Immun. 2015 Feb;44:19-27.

[4]Watson J, Brough S, Coldwell MC, Gager T, Ho M, Hunter AJ, Jerman J, Middlemiss DN, Riley GJ, Brown AM. Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors. Br J Pharmacol. 1998 Dec;125(7):1413-20.

Xanomeline/诺美林 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.36mL

17.77mL

3.55mL

1.78mL

35.53mL

7.11mL

3.55mL

Xanomeline/诺美林 技术信息

CAS号131986-45-3
分子式C14H23N3OS
分子量 281.42
SMILES Code CCCCCCOC1=NSN=C1C1=CCCN(C)C1
MDL No. MFCD00867179
别名 LY-246708
运输蓝冰
InChI Key JOLJIIDDOBNFHW-UHFFFAOYSA-N
Pubchem ID 60809
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Xanomeline | LY-246708 | AChR | AmBeed-信号通路专用抑制剂 | Xanomeline/诺美林 纯度/质量文件 | Xanomeline/诺美林 亚型比较 | Xanomeline/诺美林 生物活性 | Xanomeline/诺美林 临床数据 | Xanomeline/诺美林 参考文献 | Xanomeline/诺美林 实验方案 | Xanomeline/诺美林 技术信息

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