Xanomeline|131986-45-3|(诺美林; LY-246708)-陌孚医药/Medlife

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Xanomeline (Synonyms: 诺美林; LY-246708)

目录号: PL06875 纯度: ≥99%

CAS No. :131986-45-3

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中文名称	Xanomeline
中文别名	占诺美林;2-氯喹啉-3-硼酸;3-[4-(己基氧)-1,2,5-噻二唑-3-基]-1,2,5,6-四氢-1-甲基吡啶;5-(4-己氧基-[1,2,5]噻二唑-3-yl)-1-甲基-1,2,3,6-四氢吡啶;呫诺美林;噻诺美林;咕诺美林;3-(己氧基)-4-(1-甲基-1,2,5,6-四氢吡啶-3-基)-1,2,5-噻二唑
英文名称	Xanomeline
英文别名	3-(Hexyloxy)-4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl)-1,2,5-thiadiazole;Pyridine,3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methyl-;3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole;1,2,5-Thiadiazole,pyridine deriv.;3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine;LY 246708;Memcor;Lomeron;LY-246708;XANOMELINE;NNC-11-0232;3-(Hexyloxy);Xanomeline L-tartrate hydrate;-4-(1-methyl-1,2,5,6-tetrahydropyridin-3-yl);Xanomeline [USAN:INN];C14H23N3OS;LY246708;9ORI6L73CJ;5-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1-methyl-1,2,3,6-tetrahydropyridine;5-(4-HEXYLOXY-[1,2,5]THIADIAZOL-3-YL)-1-METHYL-1,2,3,6-TETRAHYDRO-PYRIDINE;3-(4-(Hexyloxy)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyridine;Pyridine,3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6;Xanomeline
Cas No.	131986-45-3
分子式	C₁₄H₂₃N₃Os
分子量	281.42
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Xanomeline 作为一种有效的选择性毒蕈碱 1 型和 4 型 (M1/M4) 受体激动剂可增加神经元兴奋性。Xanomeline 可用于精神分裂症等神经障碍的研究。

生物活性

Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia.

性状

Solid

IC50 & Target[1][2]

M1/M4

体外研究(In Vitro)

Xanomeline (0.1~10 μM; CNS4U) shows an overall increase in the mean firing rate. Xanomeline shows the M1 receptor is functional in hiPSC derived neurons. Xanomeline (＞1 μM) has a prolonged engagement with the receptor and produces a persistent receptor activation leading to a sustained suppression of the M-current. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Xanomeline (0.5~3 mg/kg; s.c.; 1~3 hours) induces salivation and vomiting in some monkeys.
Xanomeline shows functional dopamine antagonism and an antipsychotic-like profile. Xanomeline inhibits D-amphetamine- and (?)-apomorphine-induced behavior and do not cause extrapyramidal side effects. 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

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Kreir M, et al. Role of Kv7.2/Kv7.3 and M1 muscarinic receptors in the regulation of neuronal excitability in hiPSC-derived neurons. Eur J Pharmacol. 2019;858:172474
[2]. Shekhar A, et al. Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry. 2008;165(8):1033-1039.

溶解度数据	In Vitro: DMSO : 50 mg/mL (177.67 mM; Need ultrasonic)配制储备液

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Data Sheet

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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