GAL-021 a new intravenousPotassium Channel KCa1.1 blocker.
HazMat Fee +
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
GAL-021 is an effective BKCa-channel blocker. It inhibits KCa1.1 in GH3 cells. As a novel breathing control modulator, GAL-021 is selectively modified based on a selective modification of the almitrine pharmacophore. It increases the minute ventilation in rats and non-human primates[1][2]. GAL-021 is in development as a novel modulator for breathing control, aimed at maintaining respiratory drive and safeguarding patients from respiratory complications associated with opioids and other treatments. In GH3 cells, GAL-021 demonstrates a concentration-dependent inhibition of the single-channel activity of KCa1.1 when applied using inside-out patches. Upon testing against a panel of 12 cardiac ion channels, GAL-021 shows an inhibition of 35% or less at a concentration of 30 μM. Kinase inhibition is not significant at 10 μM. In radioligand binding assays at 30 μM, GAL-021 exhibits interactions (defined as more than 50% displacement of radioligand) with adenosine A1 (65% inhibition), A2A (79% inhibition, IC50 approximately 5μM), and A3 (93% inhibition; IC50 approximately 1 μM) receptors, and with 5-HT2B receptors (60% inhibition; IC50 approximately 30 μM)[1].
GAL-021 动物研究
Animal study
Intravenous administration of GAL-021 can alleviate respiratory depression caused by opioids in rats and non-human primates without affecting the analgesic effects in rats. The ventilatory stimulation by GAL-021 is diminished by transection of the carotid sinus nerve in rats. The ventilatory response to GAL-021 is also reduced in mice lacking the pore-forming α subunit of the KCa 1.1 channel[1].
搜索
HazMat Fee +
