Trpvicin is a potent and subtype-selective inhibitor of TRPV3 with IC50 of 0.41 and 0.22 uM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.
Trpvicin displays no significant inhibitory activities against hTRPV1, mTRPV2 and hTRPV4-6.
Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state.
Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel the channel symmetry and block the channel.
Trpvicin exhibits pharmacological potential in the inhibition of itch and hair loss in mouse models.
