AR420626 |
Catalog No.GC42831
One-Click Copy Product Info
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AR420626 is an oral active and selective agonist of free fatty acid receptor 3 (FFAR3) with an EC50 value of 2.2µM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1798310-55-0
Sample solution is provided at 25 µL, 10mM.
AR420626 is an oral active and selective agonist of free fatty acid receptor 3 (FFAR3) with an EC50 value of 2.2µM [1]. AR420626 increases the release of GLP-2 and stimulates HCO3− secretion via GLP-2 receptor activation [2]. AR420626 has been widely used to alleviate ulcer formation and gastrointestinal bleeding in rat models, and to protect gastrointestinal functions[3].
In vitro, AR420626 treatment for 48 hours significantly inhibited the proliferation of HepG2 cells, with an IC50 value of 25µM[4]. Treatment with 10µM AR420626 for 24 hours significantly enhanced the mRNA expression of TPH1 and SERT in RIN-14B cells, and also inhibited the level of IDO1[5]. Treatment with 20µM AR420626 for 24 hours significantly reduced the production of lipopolysaccharide-induced nitric oxide (NO) in RAW264.7 cells without affecting cell viability[6].
In vivo, AR420626 treatment via daily intraperitoneal injection at a dose of 26.64μg/kg for one week can improve glucose tolerance in streptozotocin (STZ)-induced diabetic mice and increase plasma insulin levels[7]. Daily oral administration of a 0.1mg/kg dose of AR420626 for 8 weeks prevented the motor disorders and loss of dopaminergic neurons in 6-hydroxydopamine (6-OHDA)-induced Parkinson's disease mice[8].
References:
[1] Lee Y J, Son S E, Im D S. Free fatty acid 3 receptor agonist AR420626 reduces allergic responses in asthma and eczema in mice[J]. International Immunopharmacology, 2024, 127: 111428.
[2] Iwasaki M, Akiba Y, Kaunitz J D. Duodenal chemosensing of short-chain fatty acids: implications for GI diseases[J]. Current gastroenterology reports, 2019, 21(8): 35.
[3] Mishra S P, Karunakar P, Taraphder S, et al. Free fatty acid receptors 2 and 3 as microbial metabolite sensors to shape host health: pharmacophysiological view[J]. Biomedicines, 2020, 8(6): 154.
[4] Mikami D, Kobayashi M, Uwada J, et al. AR420626, a selective agonist of GPR41/FFA3, suppresses growth of hepatocellular carcinoma cells by inducing apoptosis via HDAC inhibition[J]. Therapeutic advances in medical oncology, 2020, 12: 1758835920913432.
[5] Liu Z, Ling Y, Peng Y, et al. Regulation of serotonin production by specific microbes from piglet gut[J]. Journal of animal science and biotechnology, 2023, 14(1): 111.
[6] Salaga M, Bartoszek A, Binienda A, et al. Activation of free fatty acid receptor 4 affects intestinal inflammation and improves colon permeability in mice[J]. Nutrients, 2021, 13(8): 2716.
[7] Lee D H, Heo K S, Myung C S. Gαi‐coupled GPR41 activation increases Ca2+ influx in C2C12 cells and shows a therapeutic effect in diabetic animals[J]. Obesity, 2023, 31(7): 1871-1883.
[8] Hou Y, Shan C, Zhuang S, et al. Gut microbiota-derived propionate mediates the neuroprotective effect of osteocalcin in a mouse model of Parkinson’s disease[J]. Microbiome, 2021, 9(1): 34.
| Cell experiment [1]: | |
Cell lines | HepG2 cells |
Preparation Method | HepG2 cells were grown in DMEM medium with 10% (v/v) fetal bovine serum (FBS), 100μg/ml streptomycin, and 100U/ml penicillin at 37°C in 5% CO2/atmosphere. HepG2 cells (5×103 cells) were seeded on 96-well plates, incubated for 24h, and then treated with different concentrations of AR420626 (0.1, 10, 25, and 50µM) at 37°C. After 48h, cell viability was measured. |
Reaction Conditions | 0.1, 10, 25, and 50µM; 48h |
Applications | AR420626 treatment significantly reduced the cell viability of HepG2 cells in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | ICR mice |
Preparation Method | Male ICR mice (4 weeks old) were housed singly in a standard environment with food and water ad libitum. Mice were acclimated for a week before starting the experiment. Mice were intraperitoneally administered with 50mg/kg of STZ in 0.1M sodium citrate buffer (pH 4.5) once a day for 2 days. Subsequently, AR420626 (26.64μg/kg) was intraperitoneally administered once a day for 7 days. Collect samples of mouse skeletal muscles for analysis. |
Dosage form | 26.64μg/kg/day for 7 days; i.p. |
Applications | AR420626 treatment significantly enhanced skeletal muscle glycogen storage in STZ-induced diabetic mice. |
References: | |
| Cas No. | 1798310-55-0 | SDF | |
| Chemical Name | N-(2,5-dichlorophenyl)-4-(2-furanyl)-1,4,5,6,7,8-hexahydro-2-methyl-5-oxo-3-quinolinecarboxamide | ||
| Canonical SMILES | ClC1=CC(NC(C2=C(C)NC(CCCC3=O)=C3C2C4=CC=CO4)=O)=C(Cl)C=C1 | ||
| Formula | C21H18Cl2N2O3 | M.Wt | 417.3 |
| Solubility | 5mg/mL in DMSO, 2mg/mL in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3964 mL | 11.9818 mL | 23.9636 mL |
| 5 mM | 479.3 μL | 2.3964 mL | 4.7927 mL |
| 10 mM | 239.6 μL | 1.1982 mL | 2.3964 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)