TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM).

TRPC3: 4.66 μM, TRPC3:(EC50)0.45 μM , TRPC7: 1.13 μM

In the TRPC6 cells, TRPC6-IN-1 rises in a concentration dependent manner(EC50 of 4.66±0.03 μM), demonstrating a comparable activity of the compound on TRPC6 as the original lead. TRPC6-IN-1 is also tested on HEK293 cells that co-expressed μ opioid receptor (MOR) and TRPC4β, which belongs to a different subgroup of TRPC channels than TRPC3/6/7. Upon stimulation by a μ agonist, these cells show a robust increase in [Ca2+]i.In HEK293 cells . TRPC6-IN-1 also evokes whole-cell currents that express human TRPC3. TRPC6-IN-1 elicits concentration dependent current increases in the TRPC7 cells. Different from TRPC6, the currents show some desensitization in the high TRPC6-IN-1 concentrations (10 and 30 μM) at both negative and positive potentials even though the low Ca2+ (0.1 mM) bath solution is used. Nonetheless, a stepwise increase in the TRPC7 currents is still detected at <10 μM TRPC6-IN-1.