GAL-021
Based on 6 publication(s) in Google Scholar
GAL-021 is a potent BKCa-channel blocker. GAL-021 inhibits KCa1.1 in GH3 cells. GAL-021 is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 increases minute ventilation in rats and non-human primates.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.93%
- CAS. Nr.: 1380341-99-0
- Formel: C11H22N6O
- Molecular Weight:254.33
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Publications Citing Use of MedChemExpress (MCE) GAL-021
More- Pharmaceuticals (Basel). 2021 Apr 21;14(5):388. [Abstract]
- Eur J Pharmacol. 2020 Nov 15;887:173482. [Abstract]
- Biomolecules. 2020 Jan 25;10(2):188. [Abstract]
- Int J Mol Sci. 2020 Jan 5;21(1):357. [Abstract]
- BMC Pharmacol Toxicol. 2021 Jan 13;22(1):6. [Abstract]
- Oxid Med Cell Longev. 2022 Jun 20;2022:5905374. [Abstract]
Biologische Aktivität
GAL-021 is being developed as a novel breathing control modulator to preserve respiratory drive and protect patients from respiratory impairment due to opioids and other modalities. Using inside-out patches in GH3 cells, GAL-021 exerts concentration-dependent inhibition of 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 approximately 5μM), and A3 (93% I; IC50 approximately 1 μM) receptors, at 5-HT2B receptors (60% I; IC50 approximately 30 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1380341-99-0
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Appearance Solid
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Molecular Weight 254.33
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Formel C11H22N6O
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Color White to off-white
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SMILES
CCCNC1=NC(N(OC)C)=NC(NCCC)=N1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Pharmaceuticals (Basel)
Effective Activation of BKCa Channels by QO-40 (5-(Chloromethyl)-3-(Naphthalen-1-yl)-2-(Trifluoromethyl)Pyrazolo [1,5-a]pyrimidin-7(4 H)-one), Known to Be an Opener of KCNQ2/Q3 Channels. [Abstract]2021 Apr 21;14(5):388. PMID: 33919092 -
Eur J Pharmacol
High ability of zileuton ((±)-1-(1-benzo[b]thien-2-ylethyl)-1-hydroxyurea) to stimulate IK(Ca) but suppress IK(DR) and IK(M) independently of 5-lipoxygenase inhibition. [Abstract]2020 Nov 15;887:173482. PMID: 32795513 -
Biomolecules
High Efficacy by GAL-021: A Known Intravenous Peripheral Chemoreceptor Modulator that Suppresses BKCa-Channel Activity and Inhibits IK(M) or Ih. [Abstract]2020 Jan 25;10(2):188. PMID: 31991782 -
Int J Mol Sci
Characterization of Effectiveness in Concerted Ih Inhibition and IK(Ca) Stimulation by Pterostilbene (Trans-3,5-dimethoxy-4'-hydroxystilbene), a Stilbenoid. [Abstract]2020 Jan 5;21(1):357. PMID: 31948124 -
BMC Pharmacol Toxicol
Depressive effectiveness of vigabatrin (γ-vinyl-GABA), an antiepileptic drug, in intermediate-conductance calcium-activated potassium channels in human glioma cells. [Abstract]2021 Jan 13;22(1):6. PMID: 33441172 -
Oxid Med Cell Longev
Cholecystokinin Octapeptide Promotes ANP Secretion through Activation of NOX4-PGC-1 α-PPAR α/PPAR γ Signaling in Isolated Beating Rat Atria. [Abstract]2022 Jun 20;2022:5905374. PMID: 35770043
Lösungsmittel & Löslichkeit
DMSO : ≥ 30 mg/mL (117.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (8.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats: The effects of GAL-021 on mean arterial pressure (MAP) and heart rate (HR) are evaluated using IV infusions. GAL-021 (0.125 mg /kg/min for 25 min, increasing to 0.20 mg/kg/min for an additional 25 min IV) and vehicle (0.9% saline, for 50 min) are administered at a constant infusion rate (6 mL/kg/h). All rats receive additional fluid support (50:50 mixture of lactated Ringer's solution and 6% hetastarch in 0.9% saline at 4 mL/kg/min)[1]. For rat and Mouse Spirometry section, for rats, tracheal airflow is measured using flow spirometry before and after IV (femoral vein) bolus administration of GAL-021 (0.01, 0.03, 0.1, 0.3, 1.0, and 3.0 mg/kg) and vehicle (0.9% saline)[1].
Mice: The effects of GAL-021 on ventilation are also evaluated in age-matched male and female adult Slo1+/+ and Slo1-/- mice. Mice are anesthetized using 2 to 2.5% isoflurane in air[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Golder FJ, et al. Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator. Anesthesiology. 2015 Nov;123(5):1093-104. [Content Brief]
[2]. J F McLeod, et al. GAL-021, a new intravenous BKCa-channel blocker, is well tolerated and stimulates ventilation in healthy volunteers. Br J Anaesth. 2014 Nov;113(5):875-83. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.9319 mL | 19.6595 mL | 39.3190 mL | 98.2975 mL |
| 5 mM | 0.7864 mL | 3.9319 mL | 7.8638 mL | 19.6595 mL | |
| 10 mM | 0.3932 mL | 1.9659 mL | 3.9319 mL | 9.8297 mL | |
| 15 mM | 0.2621 mL | 1.3106 mL | 2.6213 mL | 6.5532 mL | |
| 20 mM | 0.1966 mL | 0.9830 mL | 1.9659 mL | 4.9149 mL | |
| 25 mM | 0.1573 mL | 0.7864 mL | 1.5728 mL | 3.9319 mL | |
| 30 mM | 0.1311 mL | 0.6553 mL | 1.3106 mL | 3.2766 mL | |
| 40 mM | 0.0983 mL | 0.4915 mL | 0.9830 mL | 2.4574 mL | |
| 50 mM | 0.0786 mL | 0.3932 mL | 0.7864 mL | 1.9659 mL | |
| 60 mM | 0.0655 mL | 0.3277 mL | 0.6553 mL | 1.6383 mL | |
| 80 mM | 0.0491 mL | 0.2457 mL | 0.4915 mL | 1.2287 mL | |
| 100 mM | 0.0393 mL | 0.1966 mL | 0.3932 mL | 0.9830 mL |
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