AR420626

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^[1][2][3][4]. 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].
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].