BPO-27 racemate是一种CFTR抑制剂，IC50为8 nM。

Bpo-27 racemate is an effective CFTR inhibitor with IC50 of 8 nM.

The R enantiomer of BPO-27 inhibits CFTR chloride conductance (IC50: 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 show 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 EC50 for ATP activation of CFTR increases from 0.27 to 1.77 mM [2].

Following bolus intraperitoneal administration of BPO-27 in mice, serum (R)-1 decays with t1/2 ≈ 1.6 h and gives sustained therapeutic concentrations in the kidney [1].

1314873-02-3

C26H18BrN3O6

548.34

BPO-27 (racemate)

DMSO:6 mg/mL (10.94 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years