BPO-27 racemate

Research use only, not for human use.

BPO-27 is a potent, metabolically stable CFTR inhibitor (IC50= 8 nM).

BPO-27 is a potent, metabolically stable CFTR inhibitor (IC50= 8 nM); shows improved potency, metabolic stability, and aqueous solubility compared to PPQ-102; prevents cyst growth with IC50 of 100 nM in embryonic kidney culture model of PKD.

The benzopyrimido-pyrrolo-oxazinedione BPO-27 is an analogue of PPQ-102, which inhibits CFTR with an IC50 of 8 nM. The R enantiomer of BPO-27 inhibits CFTR chloride conductance with an IC50 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. (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 EC50 for ATP activation of CFTR increases from 0.27 to 1.77 mM.

Following bolus interperitoneal administration in mice, serum (R)-1 decays with t1/2 ≈ 1.6 h and gives sustained therapeutic concentrations in kidney.

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Apoptosis

CFTR

CFTR

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1314873-02-3

548.34162

C26H18BrN3O6

>98% (HPLC)

DMSO: 6 mg/mL

CN1C2=C3C(OC4=C(N3C(=C2C(=O)N(C1=O)C)C5=CC=CC=C5)C=C(C=C4)C(=O)O)C6=CC=C(O6)Br

6H-Pyrimido[4',5':3,4]pyrrolo[2,1-c][1,4]benzoxazine-2-carboxylic acid, 6-(5-bromo-2-furanyl)-7,8,9,10-tetrahydro-7,9-dimethyl-8,10-dioxo-11-phenyl-, (6R)-

(-20℃)

With Ice Pack

≥ 2 years