Name | GAL-021 |
Synonyms | GAL021 GAL-021 GAL 021 GAL-021, 1380341-99-0 1,3,5-Triazine-2,4,6-triamine, N2-methoxy-N2-methyl-N4,N6-dipropyl- |
CAS | 1380341-99-0 |
Molecular Formula | C11H22N6O |
Molar Mass | 254.33 |
Density | 1.164±0.06 g/cm3(Predicted) |
Boling Point | 390.6±25.0 °C(Predicted) |
Solubility | DMSO: ≥ 30 mg/mL |
pKa | 7.07±0.10(Predicted) |
Storage Condition | -20℃ |
In vitro study | 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, IC 50 approximately 5μM), and A3 (93% I; IC 50 approximately 1 μM) receptors, at 5-HT2B receptors (60% I; IC 50 approximately 30 μM). |
In vivo study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.932 ml | 19.659 ml | 39.319 ml |
5 mM | 0.786 ml | 3.932 ml | 7.864 ml |
10 mM | 0.393 ml | 1.966 ml | 3.932 ml |
5 mM | 0.079 ml | 0.393 ml | 0.786 ml |
bioactivity | GAL-021 a new intravenous BKCa-channel blocker. |