化合物GAL021 T3557

Product Introduction
Bioactivity


英文名: GAL-021

描述: GAL-021新型静脉内BKCa-channel 阻滞剂。

激酶实验: GAL-021 is dissolved in DMSO, and final assay concentration of DMSO is 0.1% or less. The effects of GAL-021 (30 μM) on a panel of 55 receptors, transporters, and ion channels are evaluated using radioligand binding analyses. Potential kinase inhibition by GAL-021 (10 μM) is assessed using the Kinase HotSpot Screen where activity of 50 kinases is measured in the presence of adenosine triphosphate (10 μM)[1].

体外活性: 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).

体内活性: GAL-021 (i.v.) 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (196.59 mM)


关键字: KCa1.1 | minute ventilation | inhibit | BKCa | Inhibitor | KcsA | breathing control modulator | GH3 cells | Potassium Channel | GAL-021 | GAL021 | almitrine pharmacophore

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相关库: Ion Channel Inhibitor Library | Drug Repurposing Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library

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