Overview
It shows evidence of activity in preclinical tumor models and was tested in phase 1 clinical trials for the treatment of prostate cancer1-3.
- DeFalco, J. et al. (2010) Bioorg. Med. Chem. Lett. 20, 7076.
Alomone Labs D-3263 hydrochloride activates TRPM8 channels expressed in HEK-293 cells.Dose response curve for the activation of human TRPM8 by increasing concentrations of D-3263 hydrochloride (#D-195). Cells were loaded with Calcium-5 dye. Changes in intracellular Ca2+ following stimulation were detected as changes in relative fluorescence (RFU). EC50 was determined at 75 nM.
D-3263 hydrochloride, is a potent agonist of the transient receptor potential melastatin-8 (TRPM8) channel1. Activation of the channel increases Ca2+ and Na+ entry and induces cell death in TRPM8-expressing tumor cells. This agent may decrease androstanolone (DHT) levels, which may contribute to its inhibitory effects on prostate cancer and prostatic hyperplasia1.
The compound shows activity in preclinical tumor models and was tested in phase 1 clinical trials for the treatment of prostate cancer1.
TRPM8 is a Ca2+-permeable channel, a member of the 'long' or melastatin (M) group of TRP proteins and is activated by temperatures by the range of 8–28°C or by cooling compounds. The TRPM8 gene is and up-regulated in prostate cancer and other malignancies. It is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons2,3.
