Xanomeline tartrate|152854-19-8|(LY 246708 tartrate)-陌孚医药/Medlife

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Xanomeline tartrate (Synonyms: LY 246708 tartrate)

目录号: PL06856 纯度: ≥99%

CAS No. :152854-19-8

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中文名称	Xanomeline tartrate
英文名称	Xanomeline tartrate
英文别名	5-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1-methyl-1,2,3,6-tetrahydropyridine 2,3-dihydroxybutanedioate (1:1);butanedioic acid, 2,3-dihydroxy-, (2R,3R)-, compd. with 3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine (1:1);Memcor;NNC 11-0232;(2R,3R)-2,3-dihydroxybutanedioic acid,3-hexoxy-4-(1-methyl-3,6-dihydro-2H-pyridin-5-yl)-1,2,5-thiadiazole;Xanomeline tartrate
Cas No.	152854-19-8
分子式	C₁₄H₂₃N₃Os^.C₄H₆O₆
分子量	431.50
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Xanomeline (LY 246708) 是具有抗精神病样活性的毒蕈碱 M1/M4 受体的有效激动剂。Xanomeline (LY 246708) 增加神经元兴奋性。Xanomeline (LY 246708) 可用于研究精神分裂症。

生物活性

Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia.

性状

Solid

IC50 & Target[1][2]

M1/M4

体外研究(In Vitro)

Xanomeline (LY 246708) (0.1-10 μM; CNS4U) shows an overall increase in the mean firing rate. Xanomeline (LY 246708) shows the M1 receptor is functional in hiPSC derived neurons. Xanomeline (LY 246708) (＞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 (LY 246708) (0.5-3 mg/kg; s.c.; 1-3 hours) induces salivation and vomiting in some monkeys.
Xanomeline (LY 246708) shows functional dopamine antagonism and an antipsychotic-like profile.
Xanomeline (LY 246708) 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

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 : 250 mg/mL (579.37 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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