4-(4-Oxo-4H-benzo[h]chromen-2-yl)-pyridinium bisulfate

Description

UCCF-029 is a novel cystic fibrosis transmembrane conductance regulator (CFTR) activator.

Uses

UCCF-029 Free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. UCCF-029 Free base exhibits enhanced activity through benzannulation of the flavone A-ring at the 7,8-position. UCCF-029 Free base serves as a structural guide for the development of more effective flavonoid analogues. UCCF-029 Free base demonstrates improved potency compared to apigenin in activating wild-type CFTR. UCCF-029 Free base also exhibits potential for activating the mutant CFTR (G551D-CFTR) though not as robustly as apigenin.

Definition

ChEBI: 2-pyridin-4-yl-4-benzo[h][1]benzopyranone is an organic heterotricyclic compound and an organooxygen compound.

References

[1] Benzoflavone activators of the cystic fibrosis transmembrane conductance regulator: towards a pharmacophore model for the nucleotide-binding domain