Xanomeline
Based on 7 publication(s) in Google Scholar
Xanomeline, as an effective and selective muscarinic type 1 and type 4 (M1/M4) receptor agonist, increases neuronal excitability. Xanomeline can be used for the research of neurological disorders, such as schizophrenia.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.93%
- No. CAS: 131986-45-3
- Fòrmula: C14H23N3OS
- Peso molecular:281.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Xanomeline
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Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
Actividad biológica
Descripciòn
IC50 & Target
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mAChR1 |
mAChR4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BHK-21 | EC50 |
120 nM
Compound: 1
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Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M3 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
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[PMID: 20684563] |
| BHK-21 | EC50 |
140 nM
Compound: 1
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Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
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[PMID: 20684563] |
| BHK-21 | EC50 |
6.2 nM
Compound: 1
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Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
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[PMID: 20684563] |
| CHO | EC50 |
121 nM
Compound: Xanomeline
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Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
| CHO | EC50 |
142 nM
Compound: Xanomeline
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Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
| CHO | EC50 |
229 nM
Compound: Xanomeline
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Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
| CHO | EC50 |
67.3 nM
Compound: Xanomeline
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Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
| CHO-K1 | EC50 |
1.6 nM
Compound: 1
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Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
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[PMID: 20684563] |
| Fibroblast | EC50 |
134.5 nM
Compound: Xanomeline
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Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
Stimulation of phosphoinositol hydrolysis in the mouse fibroblast cell line A9L-M1 expressing Muscarinic acetylcholine receptor M1.
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[PMID: 10354408] |
| NIH3T3 | EC50 |
2.6 μM
Compound: Xanomeline
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Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells
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[PMID: 11741475] |
In Vitro
Xanomeline (0.1~10 μM; CNS4U) shows an overall increase in the mean firing rate. Xanomeline shows the M1 receptor is functional in hiPSC derived neurons. Xanomeline (>1 μM) has a prolonged engagement with the receptor and produces a persistent receptor activation leading to a sustained suppression of the M-current[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Xanomeline shows functional dopamine antagonism and an antipsychotic-like profile. Xanomeline inhibits D-amphetamine- and ( )-apomorphine-induced behavior and do not cause extrapyramidal side effects[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Cebus apella monkeys
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Dosage:0.5~3 mg/kg
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Administration:S.c.; 1~3 hours
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Result:Induced salivation and vomiting in some monkeys.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 131986-45-3
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Appearance Solid
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Peso molecular 281.42
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Fòrmula C14H23N3OS
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Color White to yellow
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SMILES
CCCCCCOC1=NSN=C1C2=CCCN(C)C2
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Synonyms
LY-246708
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Neuropsychopharmacology
Preclinical efficacy of the muscarinic agonist ML-007 in psychosis models depends on both M1 and M4 receptors. [Abstract]2025 Oct 4. PMID: 41046244
Xanomeline purchased from MedChemExpress. Usage Cited in: Neuropsychopharmacology. 2025 Oct 4. [Abstract]
Dose dependent effects of xanomeline on reversal of AIH in mice. Xanomeline (3, 6, and 10 mg/kg IP) or vehicle was administered 10 min before amphetamine (3 mg/kg IP) as two separate administrations and mice were immediately monitored for locomotion for 30 min. Data are represented as cumulative distance over 5-15 min.
Xanomeline purchased from MedChemExpress. Usage Cited in: Neuropsychopharmacology. 2025 Oct 4. [Abstract]
Dose-dependent effects of xanomeline on reversal of PCP-induced hyperlocomotion in mice. Xanomeline (3, 6, and 10 mg/kg IP) or vehicle was administered with PCP (5 mg/kg IP) as two separate administrations in rapid succession and monitored for locomotion for 30 min (n = 14-16/group, p < 0.0001). Data are presented as cumulative distance over 5-15 min.
Xanomeline purchased from MedChemExpress. Usage Cited in: Neuropsychopharmacology. 2025 Oct 4. [Abstract]
Dose-dependent reversal of AIH normalized to vehicle with comparison across wild-type (WT), M1 knockout (M1 KO), and M4 knockout (M4 KO) mice for Xanomeline 3, 6, and 10 mg/kg IP.
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Int J Mol Sci
Structural Insights into M1 Muscarinic Acetylcholine Receptor Signaling Bias between Gαq and β-Arrestin through BRET Assays and Molecular Docking. [Abstract]2023 Apr 16;24(8):7356. PMID: 37108518
Xanomeline purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Apr 16;24(8):7356. [Abstract]
Scopolamine also showed the strongest antagonistic effect on Xanomeline, with a reduction of approximately 49%, followed by Iperoxo, with a reduction of approximately 41%.
Xanomeline purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Apr 16;24(8):7356. [Abstract]
We analyzed the mean response for 100 s before or after the injection of the antagonist. Atropine showed the least potent antagonistic effect on McN-A-343, with a 12% decrease, while it had the strongest antagonistic effect on Xanomeline, with a 46% reduction.
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Synapse
Cellular-Resolution and Bulk-Fluorescence Recordings of Calcium Activity Yield Reciprocal Readouts of In Vivo Drug Efficacy. [Abstract]2025 Mar;79(2):e70011. PMID: 40013455 -
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Solvente y solubilidad
In Vitro:
Ethanol : ≥ 100 mg/mL (355.34 mM)
DMSO : 25 mg/mL (88.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 10 mg/mL (35.53 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (100.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 10 mg/mL (35.53 mM); Clear solution
This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (100.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (3.55 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (3.55 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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Neuronal voltage-sensitive dye imaging
Neuronal voltage-sensitive dye imaging detects membrane-potential-dependent optical changes from dyes associated with neuronal membranes, enabling optical recording of electrical activity from single neurons, dendrites, axons, spines, or neuronal populations in brain slices and cultured neurons. VSD signals are typically reported as fractional fluorescence or absorbance changes over baseline, such as ΔF/F or ΔI/I, and published protocols use high-speed cameras or photodiode arrays because neuronal voltage signals occur on millisecond time scales. Fast VSD imaging can be applied at two common scales: bulk staining of brain slices to measure circuit-level spatiotemporal activity, and single-cell loading or biolistic delivery to record membrane-potential transients from individual neuronal compartments. Optical signals should be interpreted as membrane-potential-related readouts, and validation by simultaneous electrophysiology or pharmacological controls is recommended when the experimen
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Cell-attached patch-clamp recording
Cell-attached patch-clamp recording measures ionic current through one or more ion channels in a small membrane patch that remains attached to an intact cell; the readout is a time-resolved current trace generated when channels in the sealed patch open and close under controlled pipette voltage or stimulus conditions. Classic applications include single acetylcholine receptor currents in frog skeletal muscle, single sodium-channel currents in cultured rat muscle cells, one-channel NMDA receptor recordings, and mechanically activated PIEZO-channel recordings. The method depends on forming a high-resistance pipette-membrane seal, commonly described as a gigaohm seal, which reduces leak and noise sufficiently to resolve picoampere-scale single-channel currents. In the cell-attached configuration, the patch membrane is not ruptured, so cytosolic composition is not directly dialyzed by the pipette solution.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kreir M, et al. Role of Kv7.2/Kv7.3 and M1 muscarinic receptors in the regulation of neuronal excitability in hiPSC-derived neurons. Eur J Pharmacol. 2019;858:172474 [Content Brief]
[2]. Shekhar A, et al. Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia. Am J Psychiatry. 2008;165(8):1033-1039. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 3.5534 mL | 17.7670 mL | 35.5341 mL | 88.8352 mL |
| 5 mM | 0.7107 mL | 3.5534 mL | 7.1068 mL | 17.7670 mL | |
| 10 mM | 0.3553 mL | 1.7767 mL | 3.5534 mL | 8.8835 mL | |
| 15 mM | 0.2369 mL | 1.1845 mL | 2.3689 mL | 5.9223 mL | |
| 20 mM | 0.1777 mL | 0.8884 mL | 1.7767 mL | 4.4418 mL | |
| 25 mM | 0.1421 mL | 0.7107 mL | 1.4214 mL | 3.5534 mL | |
| 30 mM | 0.1184 mL | 0.5922 mL | 1.1845 mL | 2.9612 mL | |
| 40 mM | 0.0888 mL | 0.4442 mL | 0.8884 mL | 2.2209 mL | |
| 50 mM | 0.0711 mL | 0.3553 mL | 0.7107 mL | 1.7767 mL | |
| 60 mM | 0.0592 mL | 0.2961 mL | 0.5922 mL | 1.4806 mL | |
| 80 mM | 0.0444 mL | 0.2221 mL | 0.4442 mL | 1.1104 mL | |
| Ethanol | 100 mM | 0.0355 mL | 0.1777 mL | 0.3553 mL | 0.8884 mL |
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