SAR7334 inhibits TRPC6, TRPC3, and TRPC7-mediated Ca2+ influx into cells (IC50s of 9.5, 282, and 226 nM, respectively) [1][2][3], while TRPC4 and TRPC5-mediated Ca2+ entry remains unaffected. At 1 μM, SAR7334 significantly blocks Ang II-evoked calcium influx in podocytes [1]. SAR7334 dose-dependently reduces TRPC6 currents with an IC50 of 7.9 nM, and at 100 nM, it substantially reduces TRPC6 currents [3].

In isolated perfused lungs from mice, SAR7334 (10?mg/kg, p.o.) inhibits TRPC6-dependent acute HPV. 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)[3].