Z3571 is a potent, highly selective and orally bioavailable TRPC6 inhibitor with binding KD of 1.62 uM, inhibits OAG-stimulated Ca2+ influx with IC50 of 31.07 nM, shows >100-fold selectivity over TRPC3 and TRPC7.
Z3571 (1 uM) specifically inhibits TRPC6-mediated Ca2+ signaling, attenuates the OAG-induced [Ca2+]i elevation in murine podocyte clone cell line MPC-5 cells, with no significant suppression of Tg- or EA-induced [Ca2+]i elevation, suggesting no detectable activity against TRPC1/4/5 channels.
Z3571 attenuates ADR-induced injury in MPC-5 cells by targeting TRPC6.
Z3571 concentration-dependently suppresses the expression and channel function of TRPC6 in ADR-injured podocytes.
Z3571 suppresses TGF-β1-induced fibrosis in HK-2 cells by targeting TRPC6
Z3571 (12.5/25/50 mg/kg)  dose-dependently restores kidney function and reduces podocyte damage in FSGS model mice.
Z3571 significantly ameliorates kidney function and reduces renal fibrosis in mice with UUO.