Two-Pore Domain (K2P) Potassium Channel Assays
Two-pore domain (K2P) channels are a subfamily of potassium channels which in humans comprises 15 members. These channels posses 2 pore-forming loops and their opening is influenced not by voltage but by a range of external influences such as neurotransmitters, second messengers, temperature and mechanical stretch. K2P channels have been shown to play key roles in excitability in the CNS, PNS, heart and muscle.
SB Drug Discovery offers a selection of K2P channel assays for HTS, lead optimization studies and selectivity profiling. Our assays have been validated by experienced in-house electrophysiologists using rigorously optimized SOPs to ensure data of the highest quality and consistency.
High throughput screening: SB offers high throughput K2P screening assays using 96 & 384 well FLIPR platforms. Example shows TREK-1 EC50 for BL 1249.
Selectivity profiling: FLIPR assays can be used to determine selectivity between closely related channels. Example shows TREK-1 IC50 for Fluoxetine.
TREK-1 electrophysiology: Left: Superimposed TREK-1 current traces under control conditions (grey line), followed by the presence of agonist BL-1249 (blue line). Right: Time-course demonstrating the stability of TREK-1 current under control conditions (white column), followed by addition of agonist BL-1249 (blue column) and finally after addition of a saturating concentration of THA (grey column).
Two-Pore Domain (K2P) Ion Channel Assays
|K2P2.1 (TREK-1)||K2P3.1 (TASK-1)||K2P4.1 (TRAAK)|
|K2P5.1 (TASK-2)||K2P9.1 (TASK-3)||K2P10.1 (TREK-2)|
|K2P13.1 (THIK-1)||K2P18.1 (TRESK)||K2P 18.1 (TRESK)|
|K2P 18.1 (TRESK)|
To discuss your next ion channel project or to receive a quote, visit our contact page or call +44 141 587 6100.