Xanomeline oxalate

Name: Xanomeline oxalate
Brand: Tocris Bioscience
SKU: 3569

Tocris Bioscience, part of Bio-Techne | Catalog # 3569

Citations (2)

COA / SDS

Functionally biased muscarinic M4 receptor agonist

Key Product Details

Description:	Functionally biased muscarinic M4 receptor agonist
Chemical Name:	3-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methylpyridine oxalate
Purity:	≥98% (HPLC)
Molecular Weight:	371.46

View Full Technical Details for Xanomeline oxalate

Technical Data
Citations

Biological Activity for Xanomeline oxalate

Xanomeline 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.

Compound Libraries for Xanomeline oxalate

Xanomeline oxalate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Xanomeline oxalate

M. Wt	371.46
Formula	C₁₄H₂₃N₃OS.C₂H₂O₄
Storage	Store at +4°C
Purity	≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Xanomeline oxalate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	3.71	10 with gentle warming
	DMSO	37.15	100

Preparing Stock Solutions for Xanomeline oxalate

The following data is based on the product molecular weight 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.

Concentration / Solvent Volume / Mass	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

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References for Xanomeline oxalate

References are publications that support the biological activity of the product.

McDonald Biased profile of xanomeline at the recombinant human M₄ muscarinic acetylcholine receptor. ACS Chem.Neurosci. 2022 PMID: 35380782
Powers Structural basis of efficacy-driven ligand selectivity at GPCRs. Nat.Chem.Biol. 2023 PMID: 36782010
Heinrich Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M₁-preferring receptor agonists. Eur.J.Pharmacol. 2009 PMID: 19168056
Stanhope The muscarinic receptor agonist xanomeline has an antipsychotic-like profile in the rat. J.Pharmacol.Exp.Ther. 2001 PMID: 11602695
Jakubik Importance and prospects for design of selective muscarinic agonists. Physiol.Res. 2008 PMID: 18481916