| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
GAL-021 sulfate targets BKCa channels (KCa1.1), which are large-conductance calcium-activated potassium channels. These channels play important roles in the regulation of neuronal excitability, smooth muscle tone, and respiratory control. By blocking BKCa channels in GH3 cells, GAL-021 sulfate modulates respiratory drive and increases minute ventilation in rats and non-human primates. The compound also inhibits the analgesic effects of opioids, suggesting a role in pain and respiratory control pathways. It is used in research on respiratory control diseases.
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| ln Vitro |
In vitro, GAL-021 sulfate inhibits KCa1.1 (BKCa) channels in GH3 cells. The compound acts as a potent BKCa channel blocker. By blocking these channels, GAL-021 sulfate modulates cellular excitability and calcium signaling. The compound is based on selective modification of the almitrine pharmacophore, which suggests it may have optimized activity and selectivity for respiratory control applications. Further in vitro studies are needed to fully characterize its channel blocking properties and selectivity.
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| ln Vivo |
In vivo, GAL-021 sulfate increases minute ventilation in rats and non-human primates. The compound inhibits the analgesic effects of opioids, indicating potential utility in managing opioid-induced respiratory depression. As a BKCa channel blocker, GAL-021 sulfate modulates respiratory drive, making it a candidate for the study of respiratory control diseases. The compound is used in research to investigate the role of BKCa channels in breathing regulation and to develop therapies for respiratory disorders.
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| Enzyme Assay |
In vitro patch-clamp electrophysiology assays are used to evaluate GAL-021 sulfate's activity on BKCa channels. The standard protocol includes whole-cell or inside-out patch-clamp recordings from GH3 cells or HEK293 cells expressing KCa1.1 channels. Varying concentrations of GAL-021 sulfate (0.1-100 µM) are applied, and channel currents are measured in response to voltage steps. The degree of current inhibition is calculated, and IC₅₀ values are determined from dose-response curves. Selectivity against other ion channels is assessed using a panel of channel types.
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| Cell Assay |
Cell-based assays for GAL-021 sulfate are conducted in GH3 cells or other cell lines expressing BKCa channels. Cells are treated with GAL-021 sulfate at concentrations ranging from 0.1-100 µM. BKCa channel activity is assessed by patch-clamp electrophysiology or by measuring changes in membrane potential using fluorescent indicators. Intracellular calcium levels are measured using fluorescent calcium indicators. Cell viability is assessed to confirm lack of cytotoxicity. The compound's effects on cellular excitability and signaling are evaluated.
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| Animal Protocol |
In vivo animal experiments for GAL-021 sulfate are conducted in rats and non-human primates. Animals are administered GAL-021 sulfate via intravenous injection or other routes. Respiratory parameters including minute ventilation, tidal volume, and respiratory rate are measured using plethysmography or other methods. The compound's effects on opioid-induced respiratory depression are assessed by co-administration with opioids. Pharmacokinetic studies are performed to determine exposure and bioavailability. The compound's safety and tolerability are evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GAL-021 sulfate are not extensively reported. As a small molecule with a molecular weight of 352.41 g/mol, the compound is expected to have moderate bioavailability. Storage: typically at -20°C. Purity is typically ≥99%. The compound is a potent BKCa channel blocker used in respiratory research. Further PK studies would be required for comprehensive characterization.
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| Toxicity/Toxicokinetics |
GAL-021 sulfate is supplied for research use only and is not intended for human administration. Toxicity data are limited, but the compound is used in research on respiratory control diseases. Standard laboratory safety precautions should be followed. No specific toxicological studies have been published. The compound should be handled with care and stored appropriately.
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| Additional Infomation |
GAL-021 sulfate (CAS 1380342-00-6) is a research compound supplied for laboratory use only. It is not an approved drug and has no marketing authorization status. The compound is a potent BKCa channel blocker that inhibits KCa1.1 in GH3 cells. It increases minute ventilation in rats and non-human primates. Purity is typically ≥99%. The compound is used for research on respiratory control and opioid-induced respiratory depression.
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| Molecular Formula |
C11H24N6O5S
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|---|---|
| Molecular Weight |
352.410460472107
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| Exact Mass |
352.152
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| CAS # |
1380342-00-6
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| Related CAS # |
GAL-021;1380341-99-0
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| PubChem CID |
86665973
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
283
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FMJQTHGXXTYHSQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H22N6O.H2O4S/c1-5-7-12-9-14-10(13-8-6-2)16-11(15-9)17(3)18-4;1-5(2,3)4/h5-8H2,1-4H3,(H2,12,13,14,15,16);(H2,1,2,3,4)
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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;sulfuric acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8376 mL | 14.1880 mL | 28.3760 mL | |
| 5 mM | 0.5675 mL | 2.8376 mL | 5.6752 mL | |
| 10 mM | 0.2838 mL | 1.4188 mL | 2.8376 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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