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Submit ReviewXanomeline oxalate is a functionally biased muscarinic M4 receptor agonist (EC50 values are 14.1 nM, 30.9 nM, 1700 nM, 1800 nM and 8500 nM at M4, M1, M2, M5 and M3 receptors respectively. Binds with similar affinity to all muscarinic acetylcholine receptors (pKi 6.7-7.7) but displays higher efficacy and efficacy-driven selectivity at M4 receptors. Displays a complex pharmacological profile: reversible and wash-resistant binding, resulting in full agonist activity at M1; delayed wash-resistant partial agonist activity at M2; and delayed wash-resistant full agonist activity at M4. Exhibits antipsychotic activity, and improves cognitive deficits and behavioral disturbances in Alzheimer's disease and schizophrenia.
Xanomeline oxalate is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 371.46 |
公式 | C14H23N3OS.C2H2O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 141064-23-5 |
PubChem ID | 18920248 |
InChI Key | ZJOUESNWCLASJP-UHFFFAOYSA-N |
Smiles | CCCCCCOC1=NSN=C1C2=CCCN(C)C2.OC(C(O)=O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 3.71 | 10 温和加热 | |
DMSO | 37.15 | 100 |
以下数据基于产品分子量 371.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.69 mL | 13.46 mL | 26.92 mL |
5 mM | 0.54 mL | 2.69 mL | 5.38 mL |
10 mM | 0.27 mL | 1.35 mL | 2.69 mL |
50 mM | 0.05 mL | 0.27 mL | 0.54 mL |
参考文献是支持产品生物活性的出版物。
Jakubik et al (2008) Importance and prospects for design of selective muscarinic agonists. Physiol.Res. 57 S39 PMID: 18481916
Heinrich et al (2009) Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists. Eur.J.Pharmacol. 605 53 PMID: 19168056
Stanhope et al (2001) The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat. J.Pharmacol.Exp.Ther. 299 782 PMID: 11602695
Powers et al (2023) Structural basis of efficacy-driven ligand selectivity at GPCRs. Nat.Chem.Biol. 19 805 PMID: 36782010
McDonald et al (2022) Biased profile of xanomeline at the recombinant human M4 muscarinic acetylcholine receptor. ACS Chem.Neurosci. 13 1206 PMID: 35380782
If you know of a relevant reference for Xanomeline oxalate, please let us know.
关键词: Xanomeline oxalate, Xanomeline oxalate supplier, Functionally, biased, M1, agonists, agonist, Muscarinic, Receptors, Acetylcholine, ACh, machr, M4, alzheimers, schizophrenia, antipsychotic, 3569, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Xanomeline oxalate 的部分引用包括:
Pasko et al (2020) Muscarinic M1 Receptors Modulate Working Memory Performance and Activity via KCNQ Potassium Channels in the Primate Prefrontal Cortex. Neuron 106 649-661.e4 PMID: 32197063
Tian et al (2016) STEP activation by Gαq coupled GPCRs opposes Src regulation of NMDA receptors containing the GluN2A subunit Scientific Reports 6 36684 PMID: 27857196
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