kca1.1

GAL-021新型静脉内BKCa-channel 阻滞剂。

NS 11021 (NS11021) 是特异性 Ca2+激活的大电导 K+(KCa1.1)通道激活剂。当浓度高于0.3 μM 时，它通过平行移动通道激活曲线产生更多负电位，以浓度依赖的方式激活 KCa1.1。

KCa1.1 channel activator-2 (化合物 3F) 是一种槲皮素衍生物，是选择性的血管 KCa1.1 channel 刺激剂。KCa1.1 channel activator-2 具有强效的肌肉松弛活性。

KCa1.1 channel activator-1 (化合物 1E) 是一种槲皮素衍生物，是选择性的血管 KCa1.1 channel 刺激剂。KCa1.1 channel activator-1 也显示 CaV1.2 channel 通道阻断活性。KCa1.1 channel activator-1 表现出较弱的肌肉松弛活性。

Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

(±)13,14-EDT是一种氧脂和腎上腺酸的代谢产物，通过细胞色素P450（CYP）途径形成。在50 nM的浓度下，它能激活分离的大鼠冠状小动脉平滑肌细胞中的大导电钙激活钾通道（KCa1.1/BK），并导致分离的猪小动脉扩张（EC50 = 12 pM）。(±)13,14-EDT还能使用TP受体激动剂U-46619预收缩的分离牛冠状动脉放松。

5(6)-DiHET is a racemic compound synthesized through the action of epoxide hydrolases on 5(6)-EET, encompassing both enantiomeric forms. It serves as a quantitative marker for 5(6)-EET, facilitating its measurement by utilizing the compound's conversion to 5(6)-δ-lactone in solution. Additionally, 5(6)-DiHET activates large-conductance calcium-activated potassium (KCa1.1 BK) channels in rat small coronary artery smooth muscle cells, supporting its biological significance in vascular regulation. It also acts as a substrate for sheep seminal vesicle COX, leading to the in vitro production of 5,6-dihydroxy prostaglandin E1 and F1α metabolites. Notably, its levels diminish in the plasma of rats subjected to a high-fat diet, indicating a potential role in the pathophysiology of hyperlipidemia.

NS309 是选择性钙依赖性钾离子通道 SK IK 的激活剂，在 BK 通道上没有激活作用。