GFB-8438 is a potent, selective TRPC5 inhibitor with IC50 of 0.18 uM (hTRPC5, Qpatch assay).
GFB-8438 inhibited the whole cell current with an IC50 of 0.28 μM comparable to the IC50 in Qpatch assay.
GFB-8438 was equipotent against TRPC4 (IC50=0.29 uM) and TRPC5.
GFB-8438 showed excellent selectivity against TRPC6, other TRP family member (TRPC3/7, TRPA1, TRPV1/2/3/4/5, and TRPM2/3/4/8).
GFB-8438 protects mouse podocytes from injury induced by protamine sulfate (PS) in vitro.
GFB-8438 demonstrated robust efficacy in the hypertensive DOCA-salt rat model without affecting blood pressure.
