IC50: 7.9 nM (TRPC6 currents)

SAR7334 inhibits TRPC6, TRPC3 and TRPC7-mediated Ca ²⁺ influx into cells with IC ₅₀ s of 9.5, 282 and 226?nM, whereas TRPC4 and TRPC5-mediated Ca ²⁺ entry is not affected. SAR7334 (1?μM) results in a major block of the Ang II-evoked calcium influx in the podocytes. SAR7334 (1 μM) has negligible effect on SOCE. SAR7334 dose-dependently reduces TRPC6 currents with an IC ₅₀ of 7.9?nM. SAR7334 (100?nM) substantially reduces TRPC6 currents.

SAR7334 (10?mg/kg, p.o.) suppresses TRPC6-dependent acute HPV in isolated perfused lungs from mice. SAR7334 demonstrates that it is suitable for chronic oral administration. In an initial short-term study, SAR7334 does not change mean arterial pressure in spontaneously hypertensive rats (SHR).