Xanomeline (Synonyms: LY-246708)

Name: Xanomeline
Brand: MedChemExpress
SKU: HY-105182
Rating: 5.0 (7 reviews)

製品番号: HY-105182 純度: 99.84%: Data Sheet SDS COA 取扱説明書
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Technical Support

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.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 131986-45-3

容量	価格（税別）	在庫状況	数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$60	在庫あり	Estimated Time of Arrival: December 31
10 mg	$100	在庫あり	Estimated Time of Arrival: December 31
25 mg	$200	在庫あり	Estimated Time of Arrival: December 31
50 mg	$320	在庫あり	Estimated Time of Arrival: December 31
100 mg	$510	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of Xanomeline:

Xanomeline-d₃ 在庫あり
Xanomeline tartrate 在庫あり
Xanomeline oxalate 在庫あり
Xanomeline-d₁₁ お問い合わせ
Xanomeline (Standard) お問い合わせ

顧客検証

•bioRxiv. 2025 Nov 21.

In Vivo Efficacy Study

Bio/Physico-chemical Assay

: 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.

: Xanomeline 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 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.

mAChR アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target

mAChR1

mAChR4

Cellular Effect

Cell Line	Type	Value	Description	References
BHK-21	EC₅₀	120 nM Compound: 1	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	[PMID: 20684563]
BHK-21	EC₅₀	140 nM Compound: 1	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	[PMID: 20684563]
BHK-21	EC₅₀	6.2 nM Compound: 1	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	[PMID: 20684563]
CHO	EC₅₀	121 nM Compound: Xanomeline	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	[PMID: 26299349]
CHO	EC₅₀	142 nM Compound: Xanomeline	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	[PMID: 26299349]
CHO	EC₅₀	229 nM Compound: Xanomeline	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	[PMID: 26299349]
CHO	EC₅₀	67.3 nM Compound: Xanomeline	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	[PMID: 26299349]
CHO-K1	EC₅₀	1.6 nM Compound: 1	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	[PMID: 20684563]
Fibroblast	EC₅₀	134.5 nM Compound: Xanomeline	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.	[PMID: 10354408]
NIH3T3	EC₅₀	2.6 μM Compound: Xanomeline	Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells Agonistic activity against M1 muscarinic receptor expressed in NIH 3T3 cells	[PMID: 11741475]

体外実験

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.

体内実験

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.

臨床実験

分子量

281.42

分子式

C₁₄H₂₃N₃OS

CAS 番号

131986-45-3

Appearance

Solid

Color

White to yellow

SMILES

CCCCCCOC1=NSN=C1C2=CCCN(C)C2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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.

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
10 mM	0.3553 mL	1.7767 mL	3.5534 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)

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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% 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.
Protocol 2

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.
Protocol 3

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.
Protocol 4

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.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (3.55 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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.

純度とドキュメンテーション

純度: 99.84%

Select Batch:

データシート (275 KB) SDS (396 KB)

COA (247 KB) HNMR (259 KB) RP-HPLC (255 KB) MS (71 KB)

取扱説明書 (2659 KB)

参考文献

[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

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

Xanomeline Related Classifications

Neurological Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

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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Xanomeline (Synonyms: LY-246708)

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Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Xanomeline Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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Xanomeline (Synonyms: LY-246708)

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Other Forms of Xanomeline:

Xanomeline 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

mAChR アイソフォーム固有の製品をすべて表示:

生物活性

純度とドキュメンテーション

参考文献

カスタマーレビュー

Xanomeline 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Xanomeline Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

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