GI-530159
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MedKoo CAT#: 471020

CAS#: 69563-88-8

Description: 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

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GI-530159
CAS# 69563-88-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 471020
Name: GI-530159
CAS#: 69563-88-8
Chemical Formula: C27H20F6N2O2
Exact Mass: 518.14
Molecular Weight: 518.459
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 190 Same day
2g USD 350 Same day
5g USD 650 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

Product Data:
Product Data
Instruction:
View handling instruction
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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 51.8 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 518.459400000000000000000000000000 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

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1. Br J Pharmacol. 2018 Jun; 175(12): 2272–2283.