Arecoline

Name: Arecoline
Brand: MedChemExpress
SKU: HY-N2364
Rating: 5.0 (5 reviews)

Cat. No.: HY-N2364 Purity: 99.84%: Data Sheet
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Arecoline, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline also can induce oxidative stress.

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

CAS No. : 63-75-2

Size	Stock	Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Liquid
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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

Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Arecoline:

Arecoline hydrobromide In-stock
Arecoline hydrochloride Get quote

5 Publications Citing Use of MCE Arecoline

Bio/Physico-chemical Assay

: Arecoline purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2025 Mar 26:294:118108. [Abstract]; Arecoline exhibited a relatively strong binding affinity to PTGS2 in vitro, with a K_D value of 10.47 μM.

: Arecoline purchased from MedChemExpress. Usage Cited in: Vet Microbiol. 2025 Dec 15:312:110818. [Abstract]; Arecoline (i.p.; single dose) stimulation led to a significant decrease in hepatic and intestinal GSH, SOD, and CAT activities and a significant increase in the MDA content, which were reversed by eFT508 (i.g.; 12 h) administration in BALB/c mice.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

nAChR/mAChR^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	10000 nM Compound: Arecoline	Stimulation of cAMP in CHO cells expressing human m2 receptor Stimulation of cAMP in CHO cells expressing human m2 receptor	[PMID: 9873644]
CHO	IC₅₀	0.115 μM Compound: Arecoline	Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells. Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.	[PMID: 11597415]
CHO	IC₅₀	115.5 μM Compound: Arecoline	Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells. Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.	[PMID: 11597415]
CHO	IC₅₀	145 μM Compound: arecoline	Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1 Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1	[PMID: 9438027]
CHO	IC₅₀	4.5 μM Compound: arecoline	Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2 Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2	[PMID: 9438027]
CHO	IC₅₀	47.5 μM Compound: arecoline	Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4 Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4	[PMID: 9438027]
CHO	IC₅₀	58 μM Compound: arecoline	Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3 Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3	[PMID: 9438027]
CHO	IC₅₀	62.5 μM Compound: arecoline	Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5 Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5	[PMID: 9438027]

In Vitro

Arecoline induces the generation of reactive oxygen species and cell cycle arrest at the G1/G0 phase in HaCaT cells without affecting the expression of p21/Cip1. Arecoline-induced epithelial cell death at higher concentrations is caused by oxidative trauma without eliciting apoptosis. Arecoline upregulates the expression of the following stress-responsive genes: hemeoxygenase-1; ferritin light chain; glucose-6-phosphate dehydrogenase; glutamatecysteine ligase catalytic subunit; and glutathione reductase^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Arecoline (0.2% in water; p.o., 2 weeks) alleviates the anxiety and depression in CFA (HY-153808)-induced mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

155.19

Formula

C₈H₁₃NO₂

CAS No.

63-75-2

Appearance

Liquid (Density: 1.0495 g/cm³)

Color

Light yellow to brown

SMILES

O=C(C1=CCCN(C)C1)OC

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

H₂O : 250 mg/mL (1610.93 mM; Need ultrasonic)

DMSO : 100 mg/mL (644.37 mM; Need ultrasonic; 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	6.4437 mL	32.2186 mL	64.4371 mL
5 mM	1.2887 mL	6.4437 mL	12.8874 mL
10 mM	0.6444 mL	3.2219 mL	6.4437 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 (protect from light). 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (16.11 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 (16.11 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 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (16.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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

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(per animal)

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(per animal)

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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: 99.84%

Select Batch:

Data Sheet (288 KB) SDS (252 KB)

COA (245 KB) HNMR (224 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. G S Thangjam, et al. Regulation of oxidative-stress responsive genes by arecoline in human keratinocytes. J Periodontal Res. 2009 Oct;44(5):673-82. [Content Brief]

[2]. Liu YJ, et, al. The pharmacology, toxicology and potential applications of arecoline: a review. Pharm Biol. 2016 Nov;54(11):2753-2760. [Content Brief]

[3]. Volgin AD, et, al. DARK Classics in Chemical Neuroscience: Arecoline. ACS Chem Neurosci. 2019 May 15;10(5):2176-2185. [Content Brief]

[4]. Kuo TM, et, al. Arecoline induces TNF-alpha production and Zonula Occludens-1 redistribution in mouse Sertoli TM4 cells. J Biomed Sci. 2014 Sep 9;21(1):93. [Content Brief]

[5]. Chen QY, et al. Inhibition of cortical synaptic transmission, behavioral nociceptive, and anxiodepressive-like responses by arecoline in adult mice. Mol Brain. 2024 Jun 17;17(1):39. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	6.4437 mL	32.2186 mL	64.4371 mL	161.0929 mL
	5 mM	1.2887 mL	6.4437 mL	12.8874 mL	32.2186 mL
	10 mM	0.6444 mL	3.2219 mL	6.4437 mL	16.1093 mL
	15 mM	0.4296 mL	2.1479 mL	4.2958 mL	10.7395 mL
	20 mM	0.3222 mL	1.6109 mL	3.2219 mL	8.0546 mL
	25 mM	0.2577 mL	1.2887 mL	2.5775 mL	6.4437 mL
	30 mM	0.2148 mL	1.0740 mL	2.1479 mL	5.3698 mL
	40 mM	0.1611 mL	0.8055 mL	1.6109 mL	4.0273 mL
	50 mM	0.1289 mL	0.6444 mL	1.2887 mL	3.2219 mL
	60 mM	0.1074 mL	0.5370 mL	1.0740 mL	2.6849 mL
	80 mM	0.0805 mL	0.4027 mL	0.8055 mL	2.0137 mL
	100 mM	0.0644 mL	0.3222 mL	0.6444 mL	1.6109 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.

Arecoline 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:

Arecoline63-75-2mAChRnAChRMuscarinic acetylcholine receptorNicotinic acetylcholine receptorsalkaloidnicotinicmuscarinicacetylcholinestimulationalertnessanxiolysisparasiticoxidativestressInhibitorinhibitorinhibit

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Arecoline

Customer Review

Other Forms of Arecoline:

Arecoline Related Antibodies

5 Publications Citing Use of MCE Arecoline

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•Related Small Molecules:

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Biological Activity

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References

Customer Review

Arecoline Related Antibodies

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Complete Stock Solution Preparation Table

Arecoline Related Classifications

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