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GAL-021 an intravenous BKCa-channel blocker.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $31 | In Stock | In Stock | |
| 5 mg | $68 | In Stock | In Stock | |
| 10 mg | $105 | In Stock | In Stock | |
| 25 mg | $197 | In Stock | In Stock | |
| 50 mg | $297 | In Stock | In Stock | |
| 100 mg | $459 | In Stock | In Stock | |
| 500 mg | $987 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $77 | In Stock | In Stock |
| Description | GAL-021 an intravenous BKCa-channel blocker. |
| In vitro | Using inside-out patches in GH3 cells, GAL-021 concentration-dependently inhibits 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: 5 μM), and A3 (93% I; IC50: 1 μM) receptors, at 5-HT2B receptors (60% I; IC50: 30 μM). |
| In vivo | GAL-021 administered intravenously (i.v.) mitigates opiate-induced respiratory depression in both rats and nonhuman primates, preserving morphine's analgesic effects in rats. Furthermore, its capacity to stimulate ventilation in rats is diminished following carotid sinus nerve transection. This ventilatory stimulation by GAL-021 is also reduced in mice devoid of the pore-forming α-subunit of the KCa 1.1 channel. |
| Kinase Assay | 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]. |
| Synonyms | GAL 021 |
| Molecular Weight | 254.33 |
| Formula | C11H22N6O |
| Cas No. | 1380341-99-0 |
| Smiles | CCCNc1nc(NCCC)nc(n1)N(C)OC |
| Relative Density. | 1.164 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (196.59 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.86 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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