[CAS NO. 1314873-02-3]  BPO-27racemate

The benzopyrimido-pyrrolo-oxazinedione BPO-27 is an analogue of PPQ-102, which inhibits CFTR with an IC ₅₀ of 8 nM. The R enantiomer of BPO-27 inhibits CFTR chloride conductance with an IC ₅₀ of 4 nM, while S enantiomer is inactive. In vitro metabolic stability in hepatic microsomes shows both enantiomers as stable, with less than 5% metabolism in 4 h ^[1] . (R)-BPO-27 binds near the canonical ATP binding site. Whole-cell patch-clamp studies shows linear CFTR currents with a voltage-independent (R)-BPO-27 block mechanism. At a concentration of (R)-BPO-27 that inhibits CFTR chloride current by 50%, the EC ₅₀ for ATP activation of CFTR increases from 0.27 to 1.77 mM ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.