Xanomeline tartrate
Based on 6 publication(s) in Google Scholar
Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity. Xanomeline (LY 246708) increases neuronal excitability. Xanomeline (LY 246708) can be used for the research of schizophrenia.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.90%
- CAS No.: 152854-19-8
- 화학식: C18H29N3O7S
- 분자량:431.50
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) Xanomeline tartrate
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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
Biological Activity
M1/M4[1]
Xanomeline (LY 246708) (0.1-10 μM; CNS4U) shows an overall increase in the mean firing rate. Xanomeline (LY 246708) shows the M1 receptor is functional in hiPSC derived neurons. Xanomeline (LY 246708) (＞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.
? Xanomeline (LY 246708) shows functional dopamine antagonism and an antipsychotic-like profile[3].
? Xanomeline (LY 246708) 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[3]
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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.
Chemical Information
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CAS No. 152854-19-8
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Appearance Solid
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분자량 431.50
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화학식 C18H29N3O7S
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Color White to off-white
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SMILES
CCCCCCOC1=NSN=C1C2=CCCN(C)C2.O[C@@H]([C@@H](C(O)=O)O)C(O)=O
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Synonyms
LY 246708 tartrate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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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 tartrate 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 tartrate 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 tartrate 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 tartrate 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 tartrate 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 -
용액&용해도
DMSO : 250 mg/mL (579.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 100 mg/mL (231.75 mM)
* "≥" 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: Saline
Solubility: ≥ 100 mg/mL (231.75 mM); Clear solution
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
순도&문서
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
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- Korean - KR (252 KB)
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Handling Instructions (2659 KB)
References
[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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.3175 mL | 11.5875 mL | 23.1750 mL | 57.9374 mL |
| 5 mM | 0.4635 mL | 2.3175 mL | 4.6350 mL | 11.5875 mL | |
| 10 mM | 0.2317 mL | 1.1587 mL | 2.3175 mL | 5.7937 mL | |
| 15 mM | 0.1545 mL | 0.7725 mL | 1.5450 mL | 3.8625 mL | |
| 20 mM | 0.1159 mL | 0.5794 mL | 1.1587 mL | 2.8969 mL | |
| 25 mM | 0.0927 mL | 0.4635 mL | 0.9270 mL | 2.3175 mL | |
| 30 mM | 0.0772 mL | 0.3862 mL | 0.7725 mL | 1.9312 mL | |
| 40 mM | 0.0579 mL | 0.2897 mL | 0.5794 mL | 1.4484 mL | |
| 50 mM | 0.0463 mL | 0.2317 mL | 0.4635 mL | 1.1587 mL | |
| 60 mM | 0.0386 mL | 0.1931 mL | 0.3862 mL | 0.9656 mL | |
| 80 mM | 0.0290 mL | 0.1448 mL | 0.2897 mL | 0.7242 mL | |
| 100 mM | 0.0232 mL | 0.1159 mL | 0.2317 mL | 0.5794 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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