1. GPCR/G Protein Neuronal Signaling
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  3. Xanomeline tartrate

Xanomeline tartrate  (Synonyms: LY 246708 tartrate)

Cat. No.: HY-105182A Purity: 99.90%
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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.

For research use only. We do not sell to patients.

CAS No. : 152854-19-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Xanomeline tartrate:

Top Publications Citing Use of Products

    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.

    Xanomeline tartrate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2023 Apr 16;24(8):7356.

    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.

    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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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1][2][3].

    IC50 & Target

    M1/M4[1]

    In Vitro

    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.

    In Vivo

    Xanomeline (LY 246708) (0.5-3 mg/kg; s.c.; 1-3 hours) induces salivation and vomiting in some monkeys[3].
    ? 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.

    Animal Model: Male Cebus apella monkeys[3]
    Dosage: 0.5-3 mg/kg
    Administration: s.c.; 1-3 hours
    Result: Induced salivation and vomiting in some monkeys.
    Molecular Weight

    431.50

    Formula

    C18H29N3O7S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CCCCCCOC1=NSN=C1C2=CCCN(C)C2.O[C@@H]([C@@H](C(O)=O)O)C(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3175 mL 11.5875 mL 23.1750 mL
    5 mM 0.4635 mL 2.3175 mL 4.6350 mL
    View the 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.

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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.

    • Protocol 1

      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.
    • Protocol 2

      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.

    • Protocol 1

      Add each solvent one by one:  Saline

      Solubility: ≥ 100 mg/mL (231.75 mM); Clear solution

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.90%

    References

    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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    Product Name:
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