[CAS NO. 69563-88-8] GI-530159

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PRODUCTS SPECIFICATIONS [69563-88-8]

Catalog

HY-W013712

Brand

MCE

CAS

69563-88-8

DESCRIPTION [69563-88-8]

Overview

MDL	MFCD00015723
Molecular Weight	518.45
Molecular Formula	C27H20F6N2O2
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

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

Summary

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 EC ₅₀ 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 EC ₅₀ s 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.

Appearance

Solid

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.

References

[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.

Synonyms

Benzenamine, 4,4′-[[2,2,2-trifluoro-1-(trifluoromethyl)ethylidene]bis(4,1-phenyleneoxy)]bis-

4,4′-[[2,2,2-Trifluoro-1-(trifluoromethyl)ethylidene]bis(4,1-phenyleneoxy)]bis[benzenamine]

2,2-Bis[4-(4-aminophenoxy)phenyl]hexafluoropropane

4,4′-Hexafluoroisopropylidenebis(p-phenyleneoxy)dianiline

4,4′-[4,4′-(Perfluoropropane-2,2-diyl)bis(4,1-phenyleneoxy)]dianiline

2,2′-Bis[4-(4-aminophenoxy)phenyl]hexafluoropropane

2,2-Bis[4-(4-aminophenoxy)phenyl]-1,1,1,3,3,3-hexafluoropropane

Bis(4-(4-aminophenoxy)phenyl)hexafluoropropane

4,4′-(Hexafluoroisopropylidene)bis[(4-aminophenoxy)benzene]

GI-530159

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