2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. GI-530159

GI-530159 

Cat. No.: HY-W013712 Purity: ≥98.0%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

GI-530159 Chemical Structure

GI-530159 Chemical Structure

CAS No. : 69563-88-8

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Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 55 In-stock
Estimated Time of Arrival: December 31
Solid
100 mg USD 50 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

Target: TREK1/2[1]
In Vitro

TREK (TWIK-related K) two pore domain potassium (K2P) channels regulate the excitability of somatosensory nociceptive neurons and mediate pain perception[1].
GI-530159 (1 µM or 10 µM) shows selectivity and activates TREK1 and TREK2 channels but shows no significant effects on TRAAK channels or K channels tested[1].
GI-530159 (0.1-30 µM) activates recombinant human TREK1 channels with EC50s of 0.8 µM and 0.9 µM from Rb efflux and electrophysiological experiments, respectively[1].
GI-530159 (1 µM) reduces rat dorsal root ganglion (DRG) neuron excitability, results in firing frequency reduction and a small hyperpolarisation of resting membrane potential (RMP)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

518.45

Appearance

Solid

Formula

C27H20F6N2O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (482.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9288 mL 9.6441 mL 19.2883 mL
5 mM 0.3858 mL 1.9288 mL 3.8577 mL
10 mM 0.1929 mL 0.9644 mL 1.9288 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

GI-53015969563-88-8GI530159GI 530159Potassium ChannelKcsAneuronexcitabilityDRGdorsal root gangliafiring frequencyanalgesictwo pore domain potassium channelsselectiveHEK293CHOtsA-201Rb effluxelectrophysiologicalresting membrane potentialRMPInhibitorinhibitorinhibit

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