TRP Channel

A 967079 is a selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively).

TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx.

GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents.

Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). Both endocannabinoids and TRPA1 may modulate gastrointestinal motility.

SKF-96365 hydrochloride is a non-selective TRP Channel blocker.

Selective TRPM4 blocker (IC50 = 20 μM in HEK293 cells). Exhibits no effect on CFTR or TRPM5 (at 0.25 and 1 mM respectively). Abolishes arrhythmias induced by hypoxia in a mouse heart model.

GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively.

TC-I 2000 is a TRPM8 channel blocker that inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells