2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Xanomeline

Xanomeline  (Synonyms: LY-246708)

Cat. No.: HY-105182 Purity: 99.52%
COA Handling Instructions

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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.

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

Xanomeline Chemical Structure

Xanomeline Chemical Structure

CAS No. : 131986-45-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 60 In-stock
10 mg USD 100 In-stock
25 mg USD 200 In-stock
50 mg USD 320 In-stock
100 mg USD 510 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Xanomeline:

Xanomeline Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Xanomeline

View All mAChR Isoform Specific Products:

View All Isoforms
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

mAChR1

 

mAChR4

 

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.

Xanomeline Related Antibodies
In Vivo

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

Animal Model: Male Cebus apella monkeys
Dosage: 0.5~3 mg/kg
Administration: S.c.; 1~3 hours
Result: Induced salivation and vomiting in some monkeys.
Clinical Trial
Molecular Weight

281.42

Formula

C14H23N3OS
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CCCCCCOC1=NSN=C1C2=CCCN(C)C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (88.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5534 mL 17.7670 mL 35.5341 mL
5 mM 0.7107 mL 3.5534 mL 7.1068 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.5 mg/mL (8.88 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (8.88 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.52%

COA (247 KB) HNMR (259 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
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. 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 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
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Xanomeline Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Xanomeline131986-45-3LY-246708LY246708LY 246708mAChRMuscarinic acetylcholine receptoreffectiveselectivemuscarinicneuronalexcitabilityneurologicaldisordersschizophreniaInhibitorinhibitorinhibit

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