Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GAL-021 an intravenous BKCa-channel blocker.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 37.00 | |
2 mg | In stock | $ 50.00 | |
5 mg | In stock | $ 90.00 | |
10 mg | In stock | $ 135.00 | |
25 mg | In stock | $ 253.00 | |
50 mg | In stock | $ 397.00 | |
100 mg | In stock | $ 589.00 | |
500 mg | In stock | $ 1,280.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 98.00 |
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 (i.v.) 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. |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (196.59 mM)
You can also refer to dose conversion for different animals. More
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