GAL-021

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型呼吸兴奋剂，可作为有效的钙激活钾 (BKCa) 通道阻滞剂。

A novel respiratory stimulant that acts as a potent calcium-activated potassium (BKCa) channel blocker blocker; reverses opioid-induced respiratory depression without compromising opioid analgesia in vivo. Respiratory insufficiencyOther Indication Phase 1 Clinical(In Vitro):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, IC50 approximately 5μM), and A3 (93% I; IC50 approximately 1 μM) receptors, at 5-HT2B receptors (60% I; IC50 approximately 30 μM).(In Vivo):Intravenously administered GAL-021 attenuates opiate-induced respiratory depression in rats and nonhuman primates without affecting 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.

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, IC50 approximately 5μM), and A3 (93% I; IC50 approximately 1 μM) receptors, at 5-HT2B receptors (60% I; IC50 approximately 30 μM).

Intravenously administered GAL-021 attenuates opiate-induced respiratory depression in rats and nonhuman primates without affecting 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.

GAL021 | GAL 021

Cell Cycle/DNA Damage

Potassium Channel

BKCa-channel

Other Indications

Other Disease

1380341-99-0

254.33198

C11H22N6O

>98% (HPLC)

DMSO: ≥ 30 mg/mL

CCCNC1=NC(N(OC)C)=NC(NCCC)=N1

1,3,5-Triazine-2,4,6-triamine, N2-methoxy-N2-methyl-N4,N6-dipropyl-

(-20℃)

With Ice Pack

≥ 2 years