BPO-27 racemat

  Cat. No.:  DC10387  
Chemical Structure
1314873-02-3
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More than 5000 active chemicals with high quality for research!
Field of application
BPO-27 racemate is a potent CFTR inhibitor with an IC50 of 8 nM.
Cas No.: 1314873-02-3
Synonyms: BPO 27 racemate; BPO27 racemate
SMILES: O=C(C1=CC=C(OC(C2=CC=C(Br)O2)C3=C(N(C)C4=O)C(C(N4C)=O)=C(C5=CC=CC=C5)N36)C6=C1)O
Formula: C26H18BrN3O6
M.Wt: 548.34
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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