861038-72-4
中文名称
A2764 dihydrochloride - TRESK inhibitor A2764
英文名称
A2764 dihydrochloride - TRESK inhibitor A2764
CAS
861038-72-4
更新日期
2024/09/03 14:18:05
分子式
C15H20Cl2N2O
分子量
315.24
MOL 文件
861038-72-4.mol
861038-72-4 结构式
基本信息
中文别名
A2764 DIHYDROCHLORIDE 英文别名
A2764 dihydrochlorideA2764 dihydrochloride - TRESK inhibitor A2764
物理化学性质
熔点184-185 °C
储存条件Inert atmosphere,Room Temperature
溶解度DMSO: 41.67 mg/mL (118.48 mM)
形态固体
颜色Light yellow to yellow
常见问题列表
生物活性
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。靶点
| Target | Value |
|
activated mTRESK channel
(Cell-free assay) | 11.8 μM |
体外研究
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.