JWU-A021

JWU-A021 is a GLP-1 secretagogue with an EC₅₀ of 1.9 μM. JWU-A021 activates the TRPA1 cation channel to promote calcium ion influx and increase intracellular calcium levels in enteroendocrine cells and TRPA1-transfected cells. By activating the TRPA1 channel, JWU-A021 stimulates the secretion of GLP-1 from intestinal enteroendocrine cells and intestinal L cells. JWU-A021 is applicable to research related to type 2 diabetes^[1]. In Vitro:JWU-A021 (3-10 μM; 30 min) potently stimulates GLP-1 secretion from mouse STC-1 intestinal enteroendocrine cells, with an EC₅₀ of 1.9 μM, inducing a ~2-fold increase over baseline at active concentrations^[1].
JWU-A021 (0.03-3 μM; measured over 300 s) induces concentration-dependent increases in [Ca²⁺]ᵢ in mouse STC-1 cells via TRPA1 channel activation, with an EC₅₀ of ~200 nM, and its dextrorotatory enantiomer is more potent than the levorotatory form^[1].
JWU-A021 (3 μM; 5 sec focal application) activates TRPA1 channels in mouse STC-1 cells, as demonstrated by induction of outwardly rectifying inward membrane currents^[1].
JWU-A021 (3 μM; 30 min) stimulates GLP-1 secretion from primary mouse intestinal L-cell cultures via TRPA1 channel activation^[1].
JWU-A021 (3 μM; 30 min) upregulates TRPA1 mRNA expression in primary mouse intestinal L-cell cultures in a TRPA1-dependent manner, increasing levels by ~40% at 3 μM for 30 minutes^[1].