GAL-021

SKU: orb1304066

Description

GAL-021

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1380341-99-0
• MW: 254.33
• Purity: 99.66%
• Formula: C₁₁H₂₂N₆O
• SMILES: CCCNc1nc(NCCC)nc(n1)N(C)OC
• Target: Potassium Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (7.86 mM);DMSO:50 mg/mL (196.59 mM)

Bioactivity

• In Vivo:
  GAL-021 administered intravenously (i.v.) mitigates opiate-induced respiratory depression in both rats and nonhuman primates, preserving morphine's analgesic effects in rats. Furthermore, its capacity to stimulate ventilation in rats is diminished following carotid sinus nerve transection. This ventilatory stimulation by GAL-021 is also reduced in mice devoid of the pore-forming α-subunit of the KCa 1.1 channel.
• 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).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

almitrine pharmacophore, BKCa, BKCa-channel, breathing control modulator, Inhibitor, GAL021, GAL-021, GAL 021, GH3 cells, minute ventilation, KcsA, KCa1.1, inhibit, PotassiumChannel, Potassium Channel

Compound Identifiers

PubChem CID

57340959