CAS: 1373268-67-7

USL311 is a synthetic small molecule that acts as an inhibitor of the ion channel TRPV4. It is also a potent activator of the G protein-coupled receptor GPR81, which may play a role in the regulation of insulin secretion. USL311 binds to the TRPV4 channel and prevents the influx of calcium ions into cells. This inhibition can be reversed by increasing concentrations of extracellular calcium ions. USL311 has shown no effect on other TRPV channels, such as TRPV1 or TRPV2, or on other receptors. TRPV4 is expressed in a number of tissues including vascular smooth muscle cells and airway epithelial cells. The activation of GPR81 by USL311 may regulate insulin secretion and glucose homeostasis in pancreatic beta cells by inhibiting the release of glucagon from alpha cells and stimulating insulin release from beta cells.

USL311 blocks CXCR4/SDF-1 interaction, inhibits tumor cell growth and migration.

USL311

6-(4-(1-Isopropylpiperidin-4-Yl)-1,4-Diazepan-1-Yl)-N-(Pyridin-4-Yl)Picolinamide