AM12

AM12 inhibits Lanthanide-evoked TRPC5 activity with an IC50 of 0.28 μM[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Research Areas >> Cardiovascular Disease

IC50: 0.28 μM (TRPC5)[1]

AM12 also inhibits TRPC5 activity evoked by the agonist (-)-Englerin A[1]. AM12 also inhibits TRPC4 channels similarly. AM12 inhibits TRPC5 and TRPC4 channels via a site accessible from the extracellular face of the membrane, acting directly on either the channel or a site closely associated with it[1]. AM12 also inhibits Ca2+ entry evoked by Gd3+. AM12 inhibits the Gd3+-evoked Ca2+ signal with an IC50 of 0.28 μM. AM12 is slightly more potent than the natural product Galangin as an inhibitor of the Gd3+-evoked signal[1].

[1]. Naylor J, et al. Natural and synthetic flavonoid modulation of TRPC5 channels. Br J Pharmacol. 2016 Feb;173(3):562-74.