| 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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| 250mg |
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| Other Sizes |
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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].
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| 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].
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| References |
| 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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