AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, GPR41) with an IC50 of 117 nM. AR420626 inhibits nicotine and serotonin-induced changes in the motility of isolated muscle strips of the rat colon and serotonin-induced faecal excretion in rats[1].
AR420626 细胞实验
Cell Line
Concentration
Treated Time
Description
References
RIN-14B cells
10 µM
24 h
To investigate the effect of AR420626 on 5-HT synthesis, results showed that AR420626 significantly upregulated TPH1 expression and promoted 5-HT production
J Anim Sci Biotechnol. 2023 Aug 5;14(1):111
Caco-2 human colonic epithelial cells
50 µM
12 h
To evaluate the effect of FFAR3 agonist on cytokine and LPS-induced IL-6 secretion. Results showed that AR420626 significantly enhanced IL-6 secretion.
Nutrients. 2021 Aug 6;13(8):2716
RAW264.7 macrophages
20 µM
24 h
To evaluate the inhibitory effect of FFAR3 agonist on LPS-induced NO production. Results showed that AR420626 significantly reduced NO secretion.
Nutrients. 2021 Aug 6;13(8):2716
HLE cells
10, 25 µM
24, 48, 72 h
Evaluate the effect of AR420626 on the proliferation of HLE cells, results showed that AR420626 significantly inhibited cell proliferation.
Ther Adv Med Oncol. 2020 Mar 20;12:1758835920913432
HepG2 cells
10, 25 µM
24, 48, 72 h
Evaluate the effect of AR420626 on the proliferation of HepG2 cells, results showed that AR420626 significantly inhibited cell proliferation.
Ther Adv Med Oncol. 2020 Mar 20;12:1758835920913432
4T1
3-30 μM
24 h
Evaluate the effect of AR420626 on 4T1 cell viability, showing significant inhibition at 3, 10, and 30 μM concentrations for 24 hours with ≈20% reduction.
Am J Cancer Res. 2024 May 15;14(5):1999-2019
MCF-7
0.1-30 μM
24 h
Evaluate the effect of AR420626 on MCF-7 cell viability, showing significant inhibition at 10 μM concentration for 24 hours.
Am J Cancer Res. 2024 May 15;14(5):1999-2019
Rat proximal colon circular muscle strips
10 μM
AR420626 inhibited nicotine- or serotonin-induced motility changes but had no effect on bethanechol-induced direct muscle contractions
Neurogastroenterol Motil. 2018 Jan;30(1):10
AR420626 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
6-hydroxydopamine-induced Parkinson's disease model
Intragastric administration
0.1 mg/kg
Once daily for 8 weeks
AR420626 mimicked the neuroprotective effects of propionate and improved motor deficits and dopaminergic neuronal loss
Microbiome. 2021 Jan 31;9(1):34
C57BL/6 mice
TNBS-induced colitis model
Intraperitoneal injection
1 mg/kg
Twice daily for 4 days
To evaluate the therapeutic effect of AR420626 on TNBS-induced colitis. Results showed no significant improvement in macroscopic and biochemical parameters of colitis.
Nutrients. 2021 Aug 6;13(8):2716
SHO nude mice
HepG2 xenograft model
Intraperitoneal injection
0.1 mg/kg (days 0-4), 0.2 mg/kg (days 7-11)
Once daily on days 0-4 and days 7-11, for 18 days
Evaluate the effect of AR420626 on the growth of HepG2 xenografts, results showed that AR420626 significantly inhibited tumor growth.
Ther Adv Med Oncol. 2020 Mar 20;12:1758835920913432
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