GSK-1702934A
TRPC3/6 activator / TRPC3 activator. In whole-cell patch-clamp experiments in HEK293 cells transduced with recombinant human TRPC3 or TRPC6, GSK-1702934A activated the TRPC3 and TRPC6 current with EC50 of 0.08 μM and 0.44 μM respectively. In the rat cardiomyocyte-like cell line H9C2 GSK-1702934A (1μM) activated TRPC6-like current and was completely blocked by GSK-417651A. It transiently increased the perfusion pressure of isolated rat heart retrogradely perfused via aortic cannulation at 1μM.1 Induces pro-arrhythmic and inotropic effects in TRPC3-overexpressing monocytes.2
Biochemicals & reagents
924377-85-5
1) Xu et al. (2013) Characterization of Small Molecule TRPC3 and TRPC6 Agonists and Antagonists; Proceedings of the Biophysical Soc.. 104(2) 454a 2) Doleschal et al. (2015) TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1.; Cardiovasc. Res., 106 163
RT
TARGET: Ion channel -- PATHWAY: Cation channel