Cat. No.: HY-N2368

Arecaidine

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Arecaidine is a GABA transport system inhibitor. Arecaidine inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine can be used in research related to neurological diseases.

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

Purity: 99.63%
CAS No.: 499-04-7
Formula: C₇H₁₁NO₂
Molecular Weight:141.17

Storage:

4°C, protect from light

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

Arecaidine Chemical Structure

CAS No.: 499-04-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Interleukin Related Isoforms :

All TGF-β Receptor Isoforms :

All TNF Receptor Isoforms :

All PPAR Isoforms :

In Vitro

Arecaidine exhibits strong binding affinity for PPAR-γ, PCK1 and TGF-β1 proteins, with binding energies of -5.1 kJ/mol, -5.6 kJ/mol and -5.6 kJ/mol^[1].
Arecaidine (0-120 μg/mL; 24-48 h) inhibits the proliferation of human oral mucosal fibroblasts (hOMF) and increases the secretion of IL-6, TGF-β and TNF-α in cells^[1].
Arecaidine (100-120 μg/mL; 48 h) downregulates the mRNA and protein expression of PPAR-γ and PCK1, while upregulates the mRNA and protein expression of TGF-β1, in human oral mucosal fibroblasts (hOMF)^[1].
Arecaidine (10 min) inhibits the uptake of GABA and β-alanine, but not that of glycine, in cat spinal cord slices, with an IC₅₀ of 89 μM for GABA and 193 μM for β-alanine^[2].
Arecaidine (10 min) inhibits the uptake of GABA and β-alanine in cat cerebellar slices, with an IC₅₀ value of 76 μM for GABA and 354 μM for β-alanine^[2].
Arecaidine (10 min) inhibits the uptake of GABA and β-alanine in rat cerebral cortex slices, with an IC₅₀ value of 122 μM for GABA and 208 μM for β-alanine^[2].
Arecaidine (0.1-100 mM; 10 min) competitively inhibits hPAT1-mediated uptake of L-[³H]proline in Caco-2 cells, with a K_i value of 7.3 mM^[3].
Arecaidine (0.1-100 mM; 10 min) inhibits hPAT1-mediated L-[³H]proline uptake in transiently transfected HeLa cells, with a K_i value of 3.8 mM^[3].

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

Cell Viability Assay^[1]

Cell Line:

human oral mucosal fibroblasts (hOMF)
Concentration:

0, 40, 60, 80, 100, 120 μg/mL
Incubation Time:

24 h; 48 h
Result:

Did not significantly alter hOMF cell viability after 24 h of treatment across all tested concentrations.
Significantly inhibited hOMF cell proliferation at 100 μg/mL and 120 μg/mL after 48 h of treatment.

ELISA Assay^[1]

Cell Line:

human oral mucosal fibroblasts (hOMF)
Concentration:

100, 120 μg/mL
Incubation Time:

48 h
Result:

Significantly elevated IL-6, TGF-β, TNF-α levels.

Real Time qPCR^[1]

Cell Line:

human oral mucosal fibroblasts (hOMF)
Concentration:

100, 120 μg/mL
Incubation Time:

48 h
Result:

Significantly downregulated PPAR-γ, PCK1, TGF-β1 mRNA expression.

Western Blot Analysis^[1]

Cell Line:

human oral mucosal fibroblasts (hOMF)
Concentration:

100 μg/mL
Incubation Time:

48 h
Result:

Significantly reduced PPAR-γ, PCK1, TGF-β1 protein expression.

In Vivo

Topical administration of arecaidine (1 mg/mL; once daily for 16 weeks) to the buccal mucosa induces oral submucous fibrosis in rats, which is characterized by reduced mouth opening, increased collagen deposition, elevated TGF-β expression, and dysregulated PPAR-γ signaling pathway^[1].
Arecaidine (0.2 M solution; electrophoretic) selectively potentiates the inhibitory effects of GABA and β-alanine on cat spinal cord neurons, and enhances the effect of GABA on cat cerebellar Purkinje cells^[2].

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

Animal Model:

Sprague-Dawley (SD) (male, 6-8 weeks old, 200 g)^[1]
Dosage:

1 mg/mL
Administration:

topical application to buccal mucosa; once daily; 16 weeks
Result:

Reduced passive mouth opening to 23.97 mm, a statistically significant reduction compared to the control group.
Increased collagen volume fraction significantly higher than the control group.
Increased TGF-β protein expression statistically significantly compared to the control group.
Identified 100 significantly differentially expressed genes, including downregulation of PPAR-γ, PCK1, pdk4, plin5, Hmgcs2, UCP3, and Angptl4, and upregulation of TGF-β1 and FOS.
Demonstrated binding energies < -5.0 kJ/mol with PPAR-γ, PCK1, and TGF-β1, indicating strong binding affinity.

Animal Model:

unspecified strain (anaesthetised with pentobarbitone sodium)^[2]
Dosage:

0.2M solution
Administration:

electrophoretic; variable duration
Result:

Selectively potentiated the inhibitory effects of GABA and β-alanine on cat spinal cord neurons, and enhanced the effect of GABA on cat cerebellar Purkinje cells.

Chemical Information

CAS No. 499-04-7
Appearance Solid
Molecular Weight 141.17
Formula C₇H₁₁NO₂
Color White to off-white
SMILES

O=C(C1=CCCN(C)C1)O
Structure Classification
- Alkaloids
- Pyridine Alkaloids
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)

Publications (1)

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Journal Impact Factor

Int J Mol Sci

Oxidative Stress and Endoplasmic Reticulum Stress Contributes to Arecoline and Its Secondary Metabolites-Induced Dyskinesia in Zebrafish Embryos. [Abstract]

2023 Mar 28;24(7):6327. PMID: 37047326

Solvent & Solubility

In Vitro:

H₂O : 250 mg/mL (1770.91 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

7.0837 mL

35.4183 mL

70.8366 mL

5 mM

1.4167 mL

7.0837 mL

14.1673 mL

10 mM

0.7084 mL

3.5418 mL

7.0837 mL

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

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

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Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Working Solution

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: PBS

Solubility: 100 mg/mL (708.37 mM); Clear solution; Need ultrasonic

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zeng F, et al. Inhibitory role of arecaidine on PPARγ signaling in oral mucosa: Mechanistic insights from transcriptome and experimental analysis. Toxicon. 2025;262:108403. [Content Brief]

[2]. Lodge D, et al. Effects of the Areca nut constituents arecaidine and guvacine on the action of GABA in the cat central nervous system. Brain Res. 1977;136(3):513-522. [Content Brief]

[3]. Voigt V, et al. Transport of the areca nut alkaloid arecaidine by the human proton-coupled amino acid transporter 1 (hPAT1). J Pharm Pharmacol. 2013;65(4):582-590. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O	1 mM	7.0837 mL	35.4183 mL	70.8366 mL	177.0915 mL
	5 mM	1.4167 mL	7.0837 mL	14.1673 mL	35.4183 mL
	10 mM	0.7084 mL	3.5418 mL	7.0837 mL	17.7091 mL
	15 mM	0.4722 mL	2.3612 mL	4.7224 mL	11.8061 mL
	20 mM	0.3542 mL	1.7709 mL	3.5418 mL	8.8546 mL
	25 mM	0.2833 mL	1.4167 mL	2.8335 mL	7.0837 mL
	30 mM	0.2361 mL	1.1806 mL	2.3612 mL	5.9030 mL
	40 mM	0.1771 mL	0.8855 mL	1.7709 mL	4.4273 mL
	50 mM	0.1417 mL	0.7084 mL	1.4167 mL	3.5418 mL
	60 mM	0.1181 mL	0.5903 mL	1.1806 mL	2.9515 mL
	80 mM	0.0885 mL	0.4427 mL	0.8855 mL	2.2136 mL
	100 mM	0.0708 mL	0.3542 mL	0.7084 mL	1.7709 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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Arecaidine

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Publications Citing Use of MedChemExpress (MCE) Arecaidine

All Interleukin Related Isoforms

All TGF-β Receptor Isoforms

All TNF Receptor Isoforms

All PPAR Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Arecaidine Related Classifications

HY-N2368 Related Classifications