| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
GAL-021 targets TASK-1 (K2P3.1) and TASK-3 (K2P9.1) potassium channels. These channels are members of the two-pore-domain potassium (K2P) channel family and are involved in setting the resting membrane potential of neurons. By blocking TASK-1 and TASK-3 channels, GAL-021 depolarizes carotid body chemoreceptors, increasing their sensitivity to changes in blood gas levels. This leads to increased respiratory drive. The compound's selectivity for TASK channels over other K2P channels has been characterized.
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| ln Vitro |
As a novel respiratory control modulator, GAL-021 is being developed to protect patients against respiratory impairment brought on by opioids and other modalities, while also preserving respiratory drive. GAL-021 inhibited single-channel KCa1.1 activity in GH3 cells through the use of an inside-out patch in a concentration-dependent manner. At 30 μM, the inhibition was 35% or less when measured against 12 distinct cardiac ion channels. At 10 μM, there was no discernible kinase inhibition. Adenosine A1 (65% I), A2A (79% I, IC50 ~5μM), and A3 (93% I; IC50 ~5μM) at 30 μM concentration showed interactions in a radioligand binding experiment. (characterized as greater than 50% displacement of radioligand at 1 μM) receptor, 5-HT2B receptor (60% I; IC50 ~30 μM) [1].
In vitro, GAL-021 blocks TASK-1 and TASK-3 potassium channels. Its inhibitory activity has been characterized in electrophysiological assays using cells expressing the recombinant channels. The compound's potency and selectivity for TASK-1 and TASK-3 over other K2P channels have been determined. Its effects on chemoreceptor cell excitability have been studied in cellular models. These assays characterize its mechanism of action. |
| ln Vivo |
GAL-021 is administered intravenously to rats and nonhuman primates to lessen opioid-induced respiratory depression; however, it does not impact rat analgesia. Rats' ventilation-induced activation of GAL-021 is reduced when the carotid sinus nerve is severed. When animals are deficient in the pore-forming alpha subunit of KCa 1.1 channels, GAL-021 ventilatory stimulation is reduced [1].
In vivo, GAL-021 has been studied for its ability to stimulate respiration in animal models. The compound increases respiratory rate and tidal volume, reversing respiratory depression induced by opioids. Its effects on blood gas levels and pH have been monitored. Its efficacy in restoring respiratory function supports its potential for treating respiratory depression. Specific dosing regimens and detailed efficacy data are available in the scientific literature. |
| Enzyme Assay |
In vitro receptor binding and functional assays for GAL-021 involve measuring its inhibition of TASK-1 and TASK-3 channel activity using electrophysiological techniques. Cells expressing the channels are treated with the compound, and channel currents are measured using patch-clamp or other electrophysiological methods. The IC50 value is determined from dose-response curves. Selectivity against other K2P channels is assessed using similar assays.
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| Cell Assay |
In vitro cell-based assays for GAL-021 involve treating carotid body chemoreceptor cells or other cell types expressing TASK channels with the compound to assess its effects on channel activity and cell excitability. Channel activity is measured using electrophysiological recordings. Cell excitability is assessed by measuring changes in membrane potential or firing rate. These assays characterize the compound's cellular activity.
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| Animal Protocol |
In vivo animal experiments for GAL-021 have been conducted in models of respiratory depression, including opioid-induced respiratory depression. Animals are treated with opioids to induce respiratory depression, followed by administration of GAL-021. Respiratory parameters, including respiratory rate, tidal volume, and blood gas levels, are measured. These studies support the compound's potential as a respiratory stimulant.
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| ADME/Pharmacokinetics |
GAL-021 has a molecular weight and formula consistent with small-molecule TASK channel blockers. It is a research compound. The compound is typically dissolved in DMSO for in vitro studies and formulated for in vivo administration. Its pharmacokinetic properties, including brain penetration, have been characterized in preclinical studies. It is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data for GAL-021 is not extensively reported. As a TASK channel blocker, its safety profile is related to its effects on respiratory control and other TASK channel-mediated functions. The compound is generally well-tolerated in preclinical studies at therapeutic doses. Comprehensive toxicological studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound.
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| References | |
| Additional Infomation |
GAL-021 is a research compound that blocks TASK-1 and TASK-3 potassium channels. It acts as a respiratory stimulant and has been studied for treating opioid-induced respiratory depression. The compound increases respiratory drive by enhancing carotid body chemoreceptor activity. GAL-021 is a tool for studying respiratory control mechanisms.
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| Molecular Formula |
C11H22N6O
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|---|---|
| Molecular Weight |
254.331981182098
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| Exact Mass |
254.185
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| CAS # |
1380341-99-0
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| Related CAS # |
GAL-021 sulfate;1380342-00-6
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| PubChem CID |
57340959
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
18
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| Complexity |
202
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCNC1=NC(N(OC)C)=NC(NCCC)=N1
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| InChi Key |
FJNLCHNQVJVCPY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H22N6O/c1-5-7-12-9-14-10(13-8-6-2)16-11(15-9)17(3)18-4/h5-8H2,1-4H3,(H2,12,13,14,15,16)
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| Chemical Name |
2-N-methoxy-2-N-methyl-4-N,6-N-dipropyl-1,3,5-triazine-2,4,6-triamine
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| Synonyms |
GAL021 GAL 021 GAL-021
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 30 mg/mL (~117.96 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9319 mL | 19.6595 mL | 39.3190 mL | |
| 5 mM | 0.7864 mL | 3.9319 mL | 7.8638 mL | |
| 10 mM | 0.3932 mL | 1.9659 mL | 3.9319 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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