Biochem/physiol Actions

GSK1702934A (GSK-2934A) is a direct activator of TRPC3 and TRPC6 ion channels with selectivity for TRPC3. In HEK293 kidney cells transduced with recombinant human TRPC3 or TRPC6, GSK1702934A activated current with an EC50 of ~ 80 nM for TRPC3 vs. 440 nM for TRPC6. It does not activate TRPV4, TRPA1, M1, M4, CaV1.2, hERG, NaV1.5, or CXCR5 receptors at concentrations ﹤10 µM. GSK1702934A has been used to study TRPC3 channels in the heart, exhibiting pro-arrhythmic, and inotropic actions in isolated Langendorff hearts from TRPC3-overexpressing mice.