Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DCPIB 是选择性可逆体积调节性阴离子通道抑制剂,抑制肿胀激活氯电流,在 CPAE 细胞中,IC50值为 4.1 μM。它能够电压依赖性激活钾离子通道 TREK1 和 TRAAK,抑制 TRESK、TASK1 和 TASK3的 IC50值分别为 0.14、0.95 和 50.72 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 369 | 现货 | ||
5 mg | ¥ 869 | 现货 | ||
10 mg | ¥ 1,270 | 现货 | ||
25 mg | ¥ 2,130 | 现货 | ||
50 mg | ¥ 3,180 | 现货 | ||
100 mg | ¥ 4,660 | 待询 | ||
200 mg | ¥ 6,630 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 898 | 现货 |
产品描述 | DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC),DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels. |
靶点活性 | TRESK:0.14 μM , TASK1:0.95 μM , TASK3:50.72 μM |
体外活性 |
DCPIB, a known specific and potent inhibitor of volume-regulated anion channels (VRAC), has been reported to activate TREK1 and TREK2 in astrocytes and in vitro recently.?In the present study, we demonstrated DCPIB also voltage dependently activated TRAAK besides TREK1/TREK2, showing DCPIB activated all TREK subfamily members.?In contrast, the compound potently inhibited several other K2P channels with no voltage dependence, including TRESK, TASK1, and TASK3.?DCPIB displayed superior selectivity toward TRESK with an IC50 of 0.14 μM, demonstrating at least 100-fold higher affinity over TREK1/TRAAK channels.?Furthermore, the impaired ion selectivity filter region greatly impaired the activating effect of DCPIB on TREK1 but not the inhibitory effect of DCPIB on TRESK.?This indicates distinct molecular determinants underlying the effect of DCPIB on TREK1 or TRESK channels.?DCPIB played diverse effects on K2P channels and could be a useful tool for further investigating structure-function studies of K2P channels. |
分子量 | 427.36 |
分子式 | C22H28Cl2O4 |
CAS No. | 82749-70-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (292.49 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.3399 mL | 11.6997 mL | 23.3995 mL | 58.4987 mL |
5 mM | 0.468 mL | 2.3399 mL | 4.6799 mL | 11.6997 mL | |
10 mM | 0.234 mL | 1.17 mL | 2.3399 mL | 5.8499 mL | |
20 mM | 0.117 mL | 0.585 mL | 1.17 mL | 2.9249 mL | |
50 mM | 0.0468 mL | 0.234 mL | 0.468 mL | 1.17 mL | |
100 mM | 0.0234 mL | 0.117 mL | 0.234 mL | 0.585 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。
DCPIB 82749-70-0 Membrane transporter/Ion channel Potassium Channel Chloride channel Cl-Channels Chloride Channel cardiomyocytes ischemia COS-7 KcsA CPAE cell Inhibitor inhibit swelling rMCAO inhibitor