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GAL-021

Catalog No. T3557   CAS 1380341-99-0
Synonyms: GAL 021

GAL-021 an intravenous BKCa-channel blocker.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
GAL-021 Chemical Structure
GAL-021, CAS 1380341-99-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 37.00
2 mg In stock $ 50.00
5 mg In stock $ 90.00
10 mg In stock $ 135.00
25 mg In stock $ 253.00
50 mg In stock $ 397.00
100 mg In stock $ 589.00
500 mg In stock $ 1,280.00
1 mL * 10 mM (in DMSO) In stock $ 98.00
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Purity: 99.73%
Purity: 99.38%
Purity: 97.71%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GAL-021 an intravenous BKCa-channel blocker.
In vitro Using inside-out patches in GH3 cells, GAL-021 concentration-dependently inhibits single-channel KCa1.1 activity. When evaluated against 12 different cardiac ion channels, inhibition is 35% or less at 30 μM. No significant kinase inhibition is observed at 10 μM. At 30 μM in the radioligand binding assays, interactions (defined as >50% radioligand displacement) are detected at adenosine A1 (65% I), A2A (79% I, IC50: 5 μM), and A3 (93% I; IC50: 1 μM) receptors, at 5-HT2B receptors (60% I; IC50: 30 μM).
In vivo GAL-021 (i.v.) attenuates opiate-induced respiratory depression in rats and nonhuman primates without affecting morphine analgesia in rats. GAL-021 ventilatory stimulation in rats is attenuated by carotid sinus nerve transection. GAL-021 ventilatory stimulation is attenuated in mice lacking the pore-forming α-subunit of the KCa 1.1 channel.
Kinase Assay GAL-021 is dissolved in DMSO, and final assay concentration of DMSO is 0.1% or less. The effects of GAL-021 (30 μM) on a panel of 55 receptors, transporters, and ion channels are evaluated using radioligand binding analyses. Potential kinase inhibition by GAL-021 (10 μM) is assessed using the Kinase HotSpot Screen where activity of 50 kinases is measured in the presence of adenosine triphosphate (10 μM)[1].
Synonyms GAL 021
Molecular Weight 254.33
Formula C11H22N6O
CAS No. 1380341-99-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (196.59 mM)

TargetMolReferences and Literature

1. Golder FJ, et al. Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator. Anesthesiology. 2015 Nov;123(5):1093-104.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Immunology/Inflammation Compound Library Potassium Channel Blocker Library ReFRAME Related Library Bioactive Compounds Library Max Anti-Cancer Compound Library Ion Channel Inhibitor Library Clinical Compound Library Drug Repurposing Compound Library

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Related compounds with same targets
Tannic acid Quinidine hydrochloride monohydrate Tetraethylammonium chloride BL-1249 DCPIB TASK-1-IN-1 CLP290 Wilfordine

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Keywords

GAL-021 1380341-99-0 Membrane transporter/Ion channel Potassium Channel KCa1.1 minute ventilation inhibit BKCa Inhibitor KcsA breathing control modulator GH3 cells GAL 021 GAL021 almitrine pharmacophore inhibitor

 

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