epithelial ion transport

GSK137647A (GSK 137647) is a selective agonist of FFA4.

ARN23765 is an F508del-CFTR corrector with an EC50 of 38 pM in human bronchial epithelial cells. It enhances the maturation and function of F508del-CFTR at the cell membrane, influencing ion transport and secretion, thereby addressing the pathological mechanisms of cystic fibrosis (CF).

Galicaftor (ABBV-2222; GLPG-2222) is a potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector that enhances CFTR protein folding and trafficking, Galicaftor is widely used in cystic fibrosis research to study CFTR rescue mechanisms, epithelial ion transport, and therapeutic correction of underlying molecular defects.

Phenamil methanesulfonate is a potent analog of Amiloride that functions as a strong and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM, Phenamil methanesulfonate also acts as a competitive inhibitor of TRPP3 and suppressing TRPP3-mediated calcium transport with an IC50 of 140 nM in Ca2+ uptake assays. Phenamil methanesulfonate robustly activates BMP signaling to promote bone repair, supporting its use in cystic fibrosis lung disease, ion channel biology, and regenerative medicine research.

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.