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Xanomeline

Catalog No. T36640   CAS 131986-45-3
Synonyms: LY-246708

Xanomeline (LY-246708) is a functionally selective M1/M4 activator used in the study of neurological disorders such as schizophrenia and has shown promising treatment in preclinical trials. Xanomeline is well absorbed orally, crosses the blood-brain barrier and undergoes extensive liver metabolism with at least six metabolites.

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Xanomeline Chemical Structure
Xanomeline, CAS 131986-45-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 80.00
25 mg In stock $ 163.00
50 mg In stock $ 263.00
100 mg In stock $ 422.00
1 mL * 10 mM (in DMSO) In stock $ 52.00
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Purity: 99.61%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Xanomeline (LY-246708) is a functionally selective M1/M4 activator used in the study of neurological disorders such as schizophrenia and has shown promising treatment in preclinical trials. Xanomeline is well absorbed orally, crosses the blood-brain barrier and undergoes extensive liver metabolism with at least six metabolites.
In vitro In binding studies pre-incubating cells for one hour with 1 μM xanomeline, but not carbachol, reduced N-[3H]methylscopolamine saturation binding affinity but not maximal receptor density in cells
[1].
In vivo Animal studies have shown the role of M4 and M1 receptors in modulating psychotic and behavioral disturbances and correction of negative and/or cognitive symptoms, respectively. The time to reach maximum plasma concentration (Tmax) for xanomeline is 2.5 hours, and maximum plasma concentration following xanomeline 150mg is 13.8ng/mL. Xanomeline is widely distributed, including to the CNS in animal studies, and the majority of the drug is excreted via the kidneys within 24 hours of administration[2].
Synonyms LY-246708
Molecular Weight 281.42
Formula C14H23N3OS
CAS No. 131986-45-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45.0 mg/mL (159.9 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Singh A. Xanomeline and Trospium: A Potential Fixed Drug Combination (FDC) for Schizophrenia-A Brief Review of Current Data. Innov Clin Neurosci. 2022 Oct-Dec;19(10-12):43-47. 2. Mirza NR, et al. Xanomeline and the antipsychotic potential of muscarinic receptor subtype selective agonists. CNS Drug Rev. 2003 Summer;9(2):159-86. 3. Andersen MB, et al. The muscarinic M1/M4 receptor agonist xanomeline exhibits antipsychotic-like activity in Cebus apella monkeys. Neuropsychopharmacology. 2003;28(6):1168-1175.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Neurotransmitter Receptor Compound Library Bioactive Compound Library Clinical Compound Library

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Propantheline bromide Oxybutynin chloride Tazomeline Olanzapine Palmatine Emraclidine Vinblastine sulfate Cyclodrine hydrochloride

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Keywords

Xanomeline 131986-45-3 Neuroscience AChR LY246708 LY 246708 LY-246708 inhibitor inhibit

 

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