Xanomeline oxalate CAS: 141064-23-5
MF: C14H23N3OS C2H2O4
MW: 371.45
A functionally selective mAChR M1 agonist.

Xanomeline oxalate (CAS 141064-23-5)

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別名: 3-[4-(Hexyloxy)-1,2,5-thiadiazol-3- yl]-1,2,5,6-tetrahydro-1-methylpyridine oxalate
アプリケーション: Xanomeline oxalate is a functionally selective mAChR M1 agonist
CAS 番号: 141064-23-5
Purity: ≥98%
Molecular Weight: 371.45
Molecular Formula: C14H23N3OS C2H2O4
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* Refer to Certificate of Analysis for lot specific data (including water content).
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Xanomeline oxalate is a functionally selective mAChR M1 agonist (EC50 values are 0.3, 5, 42, 52 and 92.5 nM at mAChR M1, mAChR M3, mAChR M5, mAChR M4 and mAChR M2 receptors, respectively). It exhibits a reversible and wash-resistant binding resulting in full agonist activity at mAChR M1, delayed wash-resistant partial agonist activity at mAChR M2 and delayed wash-resistant full agonist activity at mAChR M4.


参考文献

Stanhope et al (2001) The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat. J.Exp.Pharmacol.Ther. 299 782. Jakubik et al (2008) Importance and prospects for design of selective muscarinic agonists. Physiol.Res. 57 S39. Heinrich et al (2009) Pharmacological comparison of muscarinic ligands: historical verus more recent muscarinic M1-preferring receptor agonists. Eur.J.Pharmacol. 605 53.

Physical State :
Solid
Solubility :
Soluble in water (10 mM), DMSO (100 mM), ethanol (25 mM), DMF (1.6 mg/ml), and DMF:PBS(pH7.2)(1:9) (~0.1 mg/ml).
保存方法 :
Desiccate at 4° C
Refractive Index :
n20D ~1.54
IC50 :
Oryctolagus cuniculus: IC50 = 0.008 nM; M1 receptor: EC5050 = 0.3 nM; M3 receptor: EC5050 = 5 nM; Muscarinic acetylcholine receptor M1: IC50 = 7 nM (rat); Cavia porcellus: IC50 = > 27 µM (guinea pig)
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PubChem CID :
MDL Number :
MFCD12828778
SMILES :
CCCCCCOC1=NSN=C1C2=CCCN(C2)C.C(=O)(C(=O)O)O

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