epithelial ion transport

GSK137647A (GSK 137647) 是一种选择性FFA4激动剂，作用于人类和大小鼠FFA4的pEC50分别为6.3、6.1和6.2。

ARN23765 是一种 F508del-CFTR 校正剂，在人支气管上皮细胞中的EC50为 38 pM。它能够改善细胞膜中 F508del-CFTR 的成熟和功能，影响离子的运输与分泌，从而纠正囊性纤维化 (CF) 的病理机制。

Galicaftor（ABBV-2222；GLPG-2222）是一种高效且具有口服活性的囊性纤维化跨膜电导调节因子（CFTR）校正剂，可增强 CFTR 蛋白的折叠与转运。Galicaftor 被广泛用于囊性纤维化研究，以探讨 CFTR 功能挽救机制、上皮离子转运及潜在分子缺陷的治疗性纠正。

Phenamil methanesulfonate 是 Amiloride 的一种高效类似物，作为一种强效且较难逆转的上皮钠通道（ENaC）阻断剂，其 IC50 为 400 nM。此外，Phenamil methanesulfonate 还是 TRPP3 的竞争性抑制剂，在 Ca2+ 摄取实验中对 TRPP3 介导的钙转运抑制 IC50 为 140 nM。Phenamil methanesulfonate 可显著激活 BMP 信号通路以促进骨修复，支持其在囊性纤维化肺病、离子通道生物学及再生医学研究中的应用。

Butyrylcholine is a novel colonic ion transport regulator produced by colonic epithelial cells that stimulates nicotine and muscarinic receptors.

20-carboxy Arachidonic acid (20-COOH-AA) is the major metabolite of 20-HETE that is produced in renal tubular epithelial, endothelial, and microvascular smooth muscle cell cultures. This ω-oxidation conversion can take place using purified alcohol dehydrogenases three and four or by microsomes containing recombinant human CYP4F3B. Like 20-HETE, 20-COOH-AA inhibits ion transport in the kidneys. It also produces vasorelaxation of porcine coronary microvessels constricted with endothelin. 20-COOH-AA binds to isolated ligand binding domains of peroxisome proliferator-activated receptor α (PPARα) (Kd = 0.87 ± 0.12 μM) and PPARγ (Kd = 1.7 ± 0.5 μM), and is a dual activator of PPARα and PPARγ in a transiently transfected COS-7 cell reporter system.