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GAL-021

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Chemical Structure| 1380341-99-0 同义名 : -
CAS号 : 1380341-99-0
货号 : A239139
分子式 : C11H22N6O
纯度 : 99%+
分子量 : 254.332
MDL号 : MFCD31657265
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(117.96 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.93mL

0.79mL

0.39mL

19.66mL

3.93mL

1.97mL

39.32mL

7.86mL

3.93mL
参考文献

[1]Golder FJ, et al. Identification and Characterization of GAL-021 as a Novel Breathing Control Modulator. Anesthesiology. 2015 Nov;123(5):1093-104.

[2]J F McLeod, et al. GAL-021, a new intravenous BKCa-channel blocker, is well tolerated and stimulates ventilation in healthy volunteers. Br J Anaesth. 2014 Nov;113(5):875-83.