Methanone, (3,4-dihydro-2(1H)-isoquinolinyl)[2-[(4-methoxyphenyl)amino]-4-thiazolyl]-

GSK417651A (736945-96-3) is a TRPC blocker. In whole-cell patch-clamp experiments in HEK293 cells transfected with recombinant human TRPC3 or TRPC6, GSK417651A blocked both TRPC3 and TRPC6 current with IC50 of ~0.04 μM.1?Combined pharmacological blockade of TRPC3 and TRPC6 inhibits cardiac hypertrophy.2 Cell permeable

GSK417651A is an inhibitor of transient receptor channels 3 & 6.

1) Xu et al. (2013), Characterization of small molecule TRPC3 and TRPC6 agonists and antagonists; Biophys. J., 104 Supp 1 454a 2) Seo et al. (2014) Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy; Proc. Natl. Acad. Sci. USA, 111 1551