A2764 dihydrochloride - TRESK inhibitor A2764
| 中文名称 | A2764 dihydrochloride - TRESK inhibitor A2764 |
|---|---|
| 中文同义词 | A2764 DIHYDROCHLORIDE;化合物A2764 DIHYDROCHLORIDE;2-((5-氯喹啉-8-基)氧基)-N,N-二乙基乙胺二盐酸盐;A2764二盐酸盐 |
| 英文名称 | A2764 dihydrochloride - TRESK inhibitor A2764 |
| 英文同义词 | A2764 dihydrochloride - TRESK inhibitor A2764;A2764 dihydrochloride;2-((5-Chloroquinolin-8-yl)oxy)-N,N-diethylethanamine dihydrochloride;A2764 diHCl;nociception,A-2764 dihydrochloride,A2764,inhibit,current,A2764 dihydrochloride,KcsA,A-2764,Potassium Channel,migraine,Inhibitor,A 2764,TRESK;A2764 (hydrochloride);A2764 2HCL |
| CAS号 | 861038-72-4 |
| 分子式 | C15H20Cl2N2O |
| 分子量 | 315.24 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 861038-72-4.mol |
| 结构式 |  |
A2764 dihydrochloride - TRESK inhibitor A2764 性质
| 熔点 | 184-185 °C |
|---|---|
| 储存条件 | Inert atmosphere,Room Temperature |
| 溶解度 | 二甲基亚砜：41.67 mg/mL（118.48 mM） |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
A2764 dihydrochloride 是一种 TRESK (TWIK-related spinal cord K+ channel, K2P18.1) 的选择性抑制剂，对激活的mTRESK通道的IC50值为11.8 μM。A2764 dihydrochloride 具有探测TRESK通道在偏头痛和伤害感受中的作用的潜力。
| Target | Value |
|
activated mTRESK channel
(Cell-free assay) | 11.8 μM |
A2764 (100 µM) inhibits the background K + current by 42.8±11.5% when it applies to the oocytes expressing mTRESK.A2764 (100 µM) shows an improved inhibitory potency for activated channel with an IC 50 of activated channel in ionomycin-activated mTRESK current.The subsequent application of A2764 strongly inhibits the current (77.8±3.5%). A2764 (100 µM) inhibits the current of TRESK under resting conditions and in the activated state by 42.8±11.5% and 77.8±3.5%, respectively.