Trpvicin is a potent and subtype-selective TRPV3 inhibitor, exhibiting IC50 values of 0.41 μM for hTRPV3-WT and 0.22 μM for hTRPV3-G573S mutants. It shows only weak inhibitory effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1, and TRPM8). By binding to the VSLD-PD site, Trpvicin stabilizes the closed state of TRPV3 channels, and in the G573S mutant, it enters the central cavity, enhancing inhibition through symmetry restructuring and pore blockage. In mouse models, Trpvicin can inhibit itching and hair loss and is applicable for research related to inflammation and immunology.

Trpvicin (0-100 μM) dose-dependently inhibits currents through TRPV3-WT and hTRPV3-G573S channels expressed in HEK293T cells, achieving nearly complete inhibition at 10 μM, similar in potency to Ruthenium Red. At 10 μM for 24 hours, Trpvicin rescues the viability of HEK293T cells expressing the cytotoxic hTRPV3-G573S mutant, indicating its functional blockade of constitutively active channels. Trpvicin also dose-dependently inhibits currents of heterogeneously expressed hTRPV3-G568V and mTRPV3-G568V channels in HEK293T cells. It effectively inhibits mTRPV3-WT and gain-of-function mutant mTRPV3-G568V, with IC50 values of 0.38 μM and 0.42 μM, respectively. The potency of Trpvicin against hTRPV3 A556V, A560T, and F601A mutants is significantly reduced compared to wild-type channels (decreased by 158, 162, and 208 times, respectively), suggesting these residues are key determinants for Trpvicin binding. Trpvicin's potency against hTRPV3-G573S-F666A, hTRPV3-G573S-F666Y, and hTRPV3-G573S-T665A double mutants is decreased by 17, 12, and 16 times, respectively, indicating these residues play a crucial role in drug binding within the central cavity region beyond their primary VSLD-PD binding site.

Trpvicin, when administered intradermally at concentrations of 10 and 100 µM, 30 minutes before SLIGRL injection, significantly reduces acute scratching behavior induced by SLIGRL in mice. Administered orally at doses of 30 and 100 mg/kg, Trpvicin alleviates chronic scratching and ear swelling in mice models of dermatitis induced by MC903 when given daily for 12 days starting 5 days prior to MC903 application. Furthermore, applying 1 wt% topical Trpvicin daily for 16 days, starting from the 50th day after birth, effectively improves hair loss in both female and male Trpv3 +/G568V knock-in mice.