GI-530159

GI-530159 is a selective opener of TREK1 and TREK2 potassium channels. GI-530159 displays selectivity for TREK1/2 over TRAAK, TASK3 and other potassium channels, with an EC50 of 0.76 μM for TREK1. GI-530159 reduces rat dorsal root ganglion neuron excitability and shows potential analgesic effect[1].

Product Specifications

CAS Number

[69563-88-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gi-530159.html

Concentration

10mM

Purity

99.72

Solubility

DMSO : ≥ 100 mg/mL

Smiles

FC(C(C1=CC=C(OC2=CC=C(N)C=C2)C=C1)(C3=CC=C(OC4=CC=C(N)C=C4)C=C3)C(F)(F)F)(F)F

Molecular Formula

C27H20F6N2O2

Molecular Weight

518.45

Precautions

H302, H315, H319, H335

References & Citations

[1]Loucif AJC, et al. GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br J Pharmacol. 2018;175 (12) :2272-2283.