861038-72-4
中文名稱
A2764 dihydrochloride - TRESK inhibitor A2764
英文名稱
A2764 dihydrochloride - TRESK inhibitor A2764
CAS
861038-72-4
更新日期
2024/11/11 14:51:03
分子式
C15H20Cl2N2O
分子量
315.24
MOL 文件
861038-72-4.mol
861038-72-4 結(jié)構(gòu)式
基本信息
中文別名
A2764 DIHYDROCHLORIDE 英文別名
A2764 dihydrochlorideA2764 dihydrochloride - TRESK inhibitor A2764
物理化學(xué)性質(zhì)
熔點(diǎn)184-185 °C
儲(chǔ)存條件Inert atmosphere,Room Temperature
溶解度DMSO: 41.67 mg/mL (118.48 mM)
形態(tài)固體
顏色Light yellow to yellow
常見問題列表
生物活性
A2764 dihydrochloride 是一種 TRESK (TWIK-related spinal cord K+ channel, K2P18.1) 的選擇性抑制劑，對(duì)激活的mTRESK通道的IC50值為11.8 μM。A2764 dihydrochloride 具有探測(cè)TRESK通道在偏頭痛和傷害感受中的作用的潛力。靶點(diǎn)
| Target | Value |
|
activated mTRESK channel
(Cell-free assay) | 11.8 μM |
體外研究
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.