Cellular Effect
| Cell Line | Activity | Value | Description | Reference |
|---|---|---|---|---|
| HEK293 | IC50 | 0.413 nM | Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology | [PMID: 21128593] |
| HEK293 | IC50 | 0.8 nM | Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay | [PMID: 21128593] |
| HEK293 | IC50 | 3 nM | Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay | [PMID: 21128593] |
| HEK293 | IC50 | 4 nM | Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay | [PMID: 21128593] |