GAL-021

SKU: orb1226407

Description

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.

Key Properties

• CAS Number: 1380341-99-0
• MW: 254.33198
• Purity: >98% (HPLC)
• Formula: C₁₁H₂₂N₆O
• SMILES: CCCNC1=NC(N(OC)C)=NC(NCCC)=N1
• Target: Potassium Channel
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

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

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GAL021 | GAL 021

Quick Database Links

Gene Symbol

Potassium Channel