TRPV2 inhibitor IV2-1 is a novel TRPV2-selective blocker, inhibits 2-APB elicited typical inwardly rectifying TRPV2 currents with IC50 of 0.8 uM.
TRPV2 inhibitor IV2-1 blocks TRPV2-mediated increases in [Ca2+]i in calibrated microfluorometric single-cell analysis with IC50 of 6.3 uM.
TRPV2 inhibitor IV2-1 shows no activity against rat TRPV1, mouse TRPV3, or mouse TRPV4 channels stably expressed in HEK293 cells.
Acute modulation of TRPV2 by IV2-1 inhibits macrophage migration and phagocytosis.
TRPV2 inhibition causes significant inhibitory effects on lipopolysaccharide-induced migration of macrophages whereas TRPV2 activation promotes migration.
