(R)-Vanzacaftor is a novel BKCa channel potentiator that enhances channel activity with an EC₅₀ in the sub-micromolar range, achieving up to a threefold increase in BKCa currents in primary human bronchial epithelial cells and heterologous expression systems. Distinct from its parent compound, this enantiomer does not correct F508del CFTR function—failing to increase transepithelial Cl- current or induce band C—and does not potentiate CFTR activity. Researchers use (R)-Vanzacaftor to isolate BKCa-mediated effects in vascular reactivity and neuronal excitability studies, as it consistently vasodilates preconstricted mesenteric arteries in a paxilline-sensitive manner with no involvement of CFTR.

(R)-VX-121