MedKoo Cat#: 471020 | Name: GI-530159
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GI-530159, GI530159, GI 530159, a novel, selective, mechano-sensitive K2P channel opener. Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels.

Chemical Structure

GI-530159
GI-530159
CAS#69563-88-8 (free base)

Theoretical Analysis

MedKoo Cat#: 471020

Name: GI-530159

CAS#: 69563-88-8 (free base)

Chemical Formula: C27H20F6N2O2

Exact Mass: 518.1429

Molecular Weight: 518.46

Elemental Analysis: C, 62.55; H, 3.89; F, 21.99; N, 5.40; O, 6.17

Price and Availability

Size Price Availability Quantity
1g USD 150.00 Ready to ship
2g USD 225.00 Ready to ship
5g USD 450.00 2 weeks
10g USD 750.00 2 Weeks
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Synonym
GI-530159, GI530159, GI 530159
IUPAC/Chemical Name
4,4'-(((perfluoropropane-2,2-diyl)bis(4,1-phenylene))bis(oxy))dianiline
InChi Key
HHLMWQDRYZAENA-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H20F6N2O2/c28-26(29,30)25(27(31,32)33,17-1-9-21(10-2-17)36-23-13-5-19(34)6-14-23)18-3-11-22(12-4-18)37-24-15-7-20(35)8-16-24/h1-16H,34-35H2
SMILES Code
FC(F)(F)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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2922.39.5000
More Info
Product Data
Certificate of Analysis
Safety Data Sheet (SDS)
Biological target:
GI-530159 is a selective, mechanosensitive opener of TREK1 (K2P2.1) and TREK2 (K2P10.1) channels, with an EC50 of 0.76 μM for TREK1.
In vitro activity:
The effect of GI‐530159 on TREK channels was demonstrated using 86Rb efflux assays, whole‐cell and single‐channel patch‐clamp recordings from recombinant TREK channels. Current‐clamp recordings from cultured rat DRG neurons were used to measure the effect of GI‐530159 on neuronal excitability. For recombinant human TREK1 channels, GI‐530159 had similar low EC50 values in Rb efflux experiments and electrophysiological recordings. It activated TREK2 channels, but it had no detectable action on TRAAK channels nor any significant effect on other K channels tested. Current‐clamp recordings from cultured rat DRG neurones showed that application of GI‐530159 at 1 μM resulted in a significant reduction in firing frequency and a small hyperpolarization of resting membrane potential. This study provides pharmacological evidence for the presence of mechanosensitive TREK K2P channels in sensory neurones and suggests that development of selective K2P channel openers like GI‐530159 could aid in the development of novel analgesic agents. Reference: Br J Pharmacol. 2018 Jun; 175(12): 2272–2283. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5980259/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 51.8 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 518.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1.Loucif AJC, Saintot PP, Liu J, Antonio BM, Zellmer SG, Yoger K, Veale EL, Wilbrey A, Omoto K, Cao L, Gutteridge A, Castle NA, Stevens EB, Mathie A. GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P ) channel opener, reduces rat dorsal root ganglion neuron excitability. Br J Pharmacol. 2018 Jun;175(12):2272-2283. doi: 10.1111/bph.14098. Epub 2017 Dec 29. PMID: 29150838; PMCID: PMC5980259.
In vitro protocol:
1.Loucif AJC, Saintot PP, Liu J, Antonio BM, Zellmer SG, Yoger K, Veale EL, Wilbrey A, Omoto K, Cao L, Gutteridge A, Castle NA, Stevens EB, Mathie A. GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P ) channel opener, reduces rat dorsal root ganglion neuron excitability. Br J Pharmacol. 2018 Jun;175(12):2272-2283. doi: 10.1111/bph.14098. Epub 2017 Dec 29. PMID: 29150838; PMCID: PMC5980259.
In vivo protocol:
TBD
1. Br J Pharmacol. 2018 Jun; 175(12): 2272–2283.