Art. -Nr.: HY-116522

AR420626

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC₅₀=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca²⁺ signal-mediated glucose uptake and improve diabetes.

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Reinheit: 98.40%
CAS. Nr.: 1798310-55-0
Formel: C₂₁H₁₈Cl₂N₂O₃
Molecular Weight:417.29

Speicherung:

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

AR420626 Chemical Structure

CAS. Nr.: 1798310-55-0

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen :

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Alle HDAC Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Alle CaMK Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen :

Alle GLUT Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

AR420626 (10 μM) inhibits 100 μM nicotine-induced contraction and 10 μM nicotine-induced relaxation of rat proximal colon circular muscle strips^[1].
AR420626 (10 μM) reverses NO-mediated relaxation of circular muscles induced by 5-HT (100 μM)^[1].
AR420626 (10 and 25 µM; 48 h) inhibits the proliferation of HLE cells and HepG2 cells at a concentration of 25 µM for 48 h, and induces apoptosis of HepG2 cells and HLE cells by inhibiting HDAC-induced TNF-α^[2].
AR420626 (25 µM; 1, 3, 12 and 24 h) induces mTOR phosphorylation at the 1 h time point and for 24 h in HepG2 and HLE cells ^[2].
AR420626 (0.25, 0.5 and 1 µM; 1 h) increases Ca²⁺ influx and GLUT4 translocation via activation of CaMKII, CREB and p38 in C2C12 myotubes, thereby enhancing basal and insulin-stimulated glucose uptake^[4].

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

Cell Proliferation Assay^[2]

Cell Line:

HepG2 cells and HLE cells
Concentration:

10, 25 µM
Incubation Time:

24, 48 and 72 h
Result:

Inhibited the proliferation of HepG2 cells at 25 µM for 24 h, 10 µM and 25 µM for 48 h and 72 h, and inhibited the proliferation of HLE cells at 25 µM for 48 h, 10 µM and 25 µM for 72 h.

Western Blot Analysis^[2]

Cell Line:

HCC cells
Concentration:

10, 25 µM
Incubation Time:

48 h
Result:

Increased the expression of cleaved caspase-3 in a dose-dependent manner.
Increased cleaved caspase-8 in HCC cells in a dose-dependent manner and slightly increased cleaved caspase-9 in HepG2 cells at 25 µM.

Western Blot Analysis^[2]

Cell Line:

HCC cells
Concentration:

25 µM
Incubation Time:

1, 3, 12 and 24 h
Result:

Reduced the levels of HDAC 4-7 at 1 h and gradually decreased to 24h, reduced the levels of HDAC 1-3 at 24h, and reduced the levels of HDAC8 at 1h and gradually decreased to 24h in HepG2 cells.
Upregulated histone H3 acetylation level at 3 h and gradually increased to 24 h in HepG2 cells.

RT-PCR^[2]

Cell Line:

HCC cells
Concentration:

10, 25 µM
Incubation Time:

1, 3, 12 and 24 h
Result:

Increased the TNF-α mRNA level in HepG2 cells from 1 to 24 hours, reaching a peak at around 24 hours at a dose of 25µM, the TNF-α mRNA level in HLE cells from 1 to 24 hours was dose-dependent, reaching a peak at around 3 hours.

In Vivo

AR420626 (0.1 mg/kg, i.p.; single dose) inhibits serotonin-induced defecation volume in male Sprague-Dawley rats^[1].
AR420626 (0.1 mg/kg, i.p.; days 0-4; 0.2 mg/kg, i.p.; days 7-11) inhibits the growth of HepG2 xenografted male SHO nude mice^[2].
AR420626 (0.1 mg/kg, i.p.; administered 30 minutes before modeling) inhibits the immune response in bronchoalveolar lavage fluid (BALF) and lung tissue of the allergic asthma model induced by ovalbumins (HY-W250978) in BALB/c mice; and inhibits the skin inflammatory immune response, cervical lymph node immune response and the development of eczema symptoms in the eczema model induced by 1-chloro-2, 4-dinitrobenzene (DNCB) in BALB/c mice^[3].
AR420626 (13.32 and 26.64 μg/kg, i.p.; once a day for 7 days) at a dose of 26.64 μg/kg improves glucose tolerance by increasing plasma insulin levels and skeletal muscle glycogen content in male ICR mice with Streptozotocin (HY-13753) induced diabetes and C57BL/6 mice with high-fat diet-induced diabetes^[4].

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

Animal Model:

HepG2 xenograft model in male SHO nude mice ^[2]
Dosage:

0.1 mg/kg on days 0-4 after tumors reach 500-1000 mm³
0.2 mg/kg on days 7-11 after tumors reach 500-1000 mm³
Administration:

Intraperitoneal injection (i.p.)
Result:

Inhibited the growth of HepG2 xenograft mice, and still had an inhibitory effect on the weight of mice after stopping administration.

Animal Model:

Ovalbumin (OVA)-induced asthma induction in BALB/c mice ^[3]
Dosage:

0.1 mg/kg
Administration:

Intraperitoneal injection 30 min before OVA sensitization (D0 and D14) or 30 min before OVA challenge (D28, D29, and D30)
Result:

Suppressed the increased IL-4 and IL-17A levels.
Suppressed the increase in the number of eosinophils and total immune cells in bronchoalveolar lavage fluid (BALF).
Inhibited the increase of cytokine (IL-4, IL-13, IFN-γ and IL-17a) levels.

Animal Model:

1-chloro-2, 4-dinitrobenzene (DNCB)-induced eczema model in BALB/c mice^[3]
Dosage:

0.1 mg/kg
Administration:

Intraperitoneal injection 30 min before the DNCB challenge from day 19
Result:

Reduced the number of accumulated immune cells and mast cells, inhibited acanthosis and epidermal thickening and mast cell accumulation, and inhibited IL-17A, TSLP and IL-8 levels.
Inhibited immune responses in the cervical lymph nodes, size enlargement, and expression of inflammatory cytokines and chemokines, but did not enhance the proportion of CD4+FoxP3+ Treg cells.

Chemical Information

CAS. Nr. 1798310-55-0
Appearance Solid
Molecular Weight 417.29
Formel C₂₁H₁₈Cl₂N₂O₃
Color Off-white to light yellow
SMILES

ClC1=CC(NC(C2=C(NC(CCC3)=C(C2C4=CC=CO4)C3=O)C)=O)=C(C=C1)Cl
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (4)

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Journal Impact Factor

Cancer Cell

Fusobacterium nucleatum facilitates anti-PD-1 therapy in microsatellite stable colorectal cancer. [Abstract]

2024 Oct 14;42(10):1729-1746.e8. PMID: 39303724
ISME J

Ginsenoside Rg3 enriches SCFA-producing commensal bacteria to confer protection against enteric viral infection via the cGAS-STING-type I IFN axis. [Abstract]

2023 Dec;17(12):2426-2440. PMID: 37950067
J Pharm Anal

2026 Mar 19.
J Anim Sci Biotechnol

Regulation of serotonin production by specific microbes from piglet gut. [Abstract]

2023 Aug 5;14(1):111. PMID: 37542282

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (47.93 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)

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

2.3964 mL

11.9821 mL

23.9641 mL

5 mM

0.4793 mL

2.3964 mL

4.7928 mL

10 mM

0.2396 mL

1.1982 mL

2.3964 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 90% (20% SBE-β-CD in Saline)

Solubility: 2 mg/mL (4.79 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 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 (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (4.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2 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 (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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)

Verweise

[1]. Kaji I, et al. Free fatty acid receptor 3 activation suppresses neurogenic motility in rat proximal colon. Neurogastroenterol Motil. 2018 Jan;30(1):10.1111/nmo.13157. [Content Brief]

[2]. Mikami, et al. AR420626, a selective agonist of GPR41/FFA3, suppresses growth of hepatocellular carcinoma cells by inducing apoptosis via HDAC inhibition. Therapeutic Advances in Medical Oncology 12 (2020): 1758835920913432. [Content Brief]

[3]. Ye-Ji Lee, et al. Free fatty acid 3 receptor agonist AR420626 reduces allergic responses in asthma and eczema in mice. International Immunopharmacology 127 (2024): 111428. [Content Brief]

[4]. Do‐Hyung, et al. Gαi‐coupled GPR41 activation increases Ca2+ influx in C2C12 cells and shows a therapeutic effect in diabetic animals. Obesity 31.7 (2023): 1871-1883. [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

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	2.3964 mL	11.9821 mL	23.9641 mL	59.9104 mL
	5 mM	0.4793 mL	2.3964 mL	4.7928 mL	11.9821 mL
	10 mM	0.2396 mL	1.1982 mL	2.3964 mL	5.9910 mL
	15 mM	0.1598 mL	0.7988 mL	1.5976 mL	3.9940 mL
	20 mM	0.1198 mL	0.5991 mL	1.1982 mL	2.9955 mL
	25 mM	0.0959 mL	0.4793 mL	0.9586 mL	2.3964 mL
	30 mM	0.0799 mL	0.3994 mL	0.7988 mL	1.9970 mL
	40 mM	0.0599 mL	0.2996 mL	0.5991 mL	1.4978 mL

Keywords

AR420626

4 Cited Publications

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AR420626

Apoptosis Compound Library

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Publications Citing Use of MedChemExpress (MCE) AR420626

Alle Free Fatty Acid Receptor Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Alle CaMK Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle Epigenetic Reader Domain Isoform-spezifische Produkte anzeigen

Alle GLUT Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AR420626 Related Classifications

HY-116522 Related Classifications