Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GAL-021新型静脉内BKCa-channel 阻滞剂。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 335 | 现货 | ||
2 mg | ¥ 478 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,260 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,420 | 现货 | ||
500 mg | ¥ 11,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 861 | 现货 |
产品描述 | GAL-021 an intravenous BKCa-channel blocker. |
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. |
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]. |
别名 | GAL 021 |
分子量 | 254.33 |
分子式 | C11H22N6O |
CAS No. | 1380341-99-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (196.59 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.9319 mL | 19.6595 mL | 39.319 mL | 98.2975 mL |
5 mM | 0.7864 mL | 3.9319 mL | 7.8638 mL | 19.6595 mL | |
10 mM | 0.3932 mL | 1.9659 mL | 3.9319 mL | 9.8297 mL | |
20 mM | 0.1966 mL | 0.983 mL | 1.9659 mL | 4.9149 mL | |
50 mM | 0.0786 mL | 0.3932 mL | 0.7864 mL | 1.9659 mL | |
100 mM | 0.0393 mL | 0.1966 mL | 0.3932 mL | 0.983 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GAL-021 1380341-99-0 Membrane transporter/Ion channel Potassium Channel KCa1.1 minute ventilation inhibit BKCa Inhibitor KcsA breathing control modulator GH3 cells GAL 021 GAL021 almitrine pharmacophore inhibitor