Colivin is a potent, selective and orally bioactive TRPV3 inhibitor/antagonist, suppresses hTRPV3 activity with IC50 of 0.23 uM in Fluorescence-based Ca2+ influx assays, inhibits hTRPV3 and mTRPV3 equally.
Colivin concentration-dependently suppresses 2-APB (100 μM)-induced outward and inward currents in HEK-293 cells transiently expressing hTRPV3 with IC50 values of 0.24  μM and 0.20  μM at +100 and −100 mV, respectively.
Colivin has IC50 values of 0.24  μM and 0.20 μM at +100 and −100  mV, respectively, in HEK-293 cells transiently expressing mTRPV3.
Colivin acts as a non-competitive inhibitor of TRPV3.
Colivin has no significant effect on Ca2+ influx mediated by hTRPV1, mTRPV2, hTRPV4, hTRPA1, and hTRPM8 at 10 uM.
Colivin binds to the vanilloid site of hTRPV3.
Colivin stabilizes TRPV3 in a non-conducting conformation.
Colivin (10 mg/kg, intragastric administration) ameliorates DSS-induced ulcerative colitis (UC) in mice.