Overview
- Parks, D.J. et al. (2011) J. Med. Chem. 54, 233.
Alomone Labs TC-I 2014 inhibits TRPM8 channels expressed in HEK-293 cells.Dose response curve of TRPM8 inhibition by TC-I 2014 (#T-200), showing nearly complete inhibition at 1 µM. Cells were loaded with Calcium-5 dye, incubated for 10 min with increasing concentrations of TC-I 2014, and activated by 30 nM Icilin. Changes in intracellular Ca2+ following agonist application were detected as changes in 485 nm/525 nm fluorescence (RFU).
TC-I 2014 is a selective TRPM8 channel blocker. The compound shows high affinity towards TRPM8 and exhibits in vitro functional activity and good oral efficacy in an inflammatory model of neuropathic pain1. TC-I 2014 inhibits canine, rat, and human TRPM8 mediated Ca2+ influx functional assays with IC50 values of 0.8, 4.0, and 3.0 nM, respectively1.
TRPM8 channel is a member of the TRP channels superfamily. TRPM8 is a Ca2+-permeable, nonselective cation channel that is activated by temperatures in the range of 8–28°C and by chemical agonists such as menthol and icilin. The channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons. Its expression is up-regulated in prostate cancer and other malignancies1,2.
