GAL-021 |
Catalog No.GC18210
One-Click Copy Product Info
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GAL-021 is a large-conductance Ca2+-activated potassium channel (BKCa/KCa1.1) blocker.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1380341-99-0
Sample solution is provided at 25 µL, 10mM.
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GAL-021 a new intravenous BKCa-channel blocker.
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].
Intravenously administered GAL-021 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[1].
References:
[1]. Golder FJ, et al. Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator. Anesthesiology. 2015 Nov;123(5):1093-104.
Kinase experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Golder FJ, et al. Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator. Anesthesiology. 2015 Nov;123(5):1093-104. | |
| Cas No. | 1380341-99-0 | SDF | |
| Chemical Name | N2-methoxy-N2-methyl-N4,N6-dipropyl-1,3,5-triazine-2,4,6-triamine | ||
| Canonical SMILES | CN(OC)C1=NC(NCCC)=NC(NCCC)=N1 | ||
| Formula | C11H22N6O | M.Wt | 254.3 |
| Solubility | DMSO : ≥ 30 mg/mL (117.96 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9324 mL | 19.6618 mL | 39.3236 mL |
| 5 mM | 786.5 μL | 3.9324 mL | 7.8647 mL |
| 10 mM | 393.2 μL | 1.9662 mL | 3.9324 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)