Xanomeline oxalate

Catalog # Availability Size / Price Qty
3569/10
3569/50
Xanomeline oxalate | CAS No. 141064-23-5 | mAChR M1 Agonists
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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%

Product Details
Citations (2)
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Reviews

Biological Activity

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.

Technical Data

M.Wt:
371.46
Formula:
C14H23N3OS.C2H2O4
Solubility:
Soluble to 10 mM in water with gentle warming and to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
141064-23-5

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.

Background References

  1. Multiplex single-molecule interaction profiling of DNA-barcoded proteins.
    Gu, Liangcai, Li, Chao, Aach, John, Hill, David E, Vidal, Marc, Church, George M
    Nature, 2014;515(7528):554-7.
  2. Importance and prospects for design of selective muscarinic agonists.
    Jakubik et al.
    Physiol.Res., 2008;57:S39
  3. Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists.
    Heinrich et al.
    Eur.J.Pharmacol., 2009;605:53

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Citations for Xanomeline oxalate

The citations listed below are publications that use Tocris products. Selected citations for Xanomeline oxalate include:

2 Citations: Showing 1 - 2

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