A potent, selective and orally available TRPM8 channel inhibitor with IC50 of 8.3 nM (hTRPM8); inhibits rTRPM8 wiht IC50 of 5.8 nMdisplays no significant activities against TRPA1, TRPV4 and TRPV1 (IC50>3 uM); demonstrates excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats; also reduces the invasion potential of oral squamous carcinoma cell lines.
