General description
A cell-permeable pyrimido-pyrrolo-quinoxalinedione (PPQ) compound that targets the intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR-mediated chloride current in a reversible and voltage-independent manner. Single channel recordings of CFTR-expressing FRT cells upon forskolin (Cat. No. 344270) and IBMX (Cat. No. 410957) stimulation indicate that the nature of PPQ-102 inhibition is due to a stabilization of the channels in a closed state (7.8- vs. 0.4-fold increase of mean channel close vs. open time, respectively, with 1 µM PPQ-102). PPQ-102 at 5 µM is shown to completely prevent Sp-8-Br-cAMP- (Cat. No. 116818) induced cysts formation and reduce the size of preformed cysts in an ex vivo murine neonatal kidney organ culture.
A cell-permeable pyrimido-pyrrolo-quinoxalinedione (PPQ) compound that targets the intracellular nucleotide binding domain(s) of CFTR and inhibits CFTR-mediated chloride current in a reversible and voltage-independent manner. Single channel recordings of CFTR-expressing FRT cells upon forskolin (Cat. No. 344270) and IBMX (Cat. No. 410957) stimulation indicate that the nature of PPQ-102 inhibition is due to a stabilization of the channels in a closed state (7.8- vs. 0.4-fold increase of mean channel close vs. open time, respectively, with 1 µM PPQ-102). PPQ-102 at 5 µM is shown to completely prevent Sp-8-Br-cAMP- (Cat. No. 116818) induced cysts formation and reduce the size of preformed cysts in an ex vivo murine neonatal kidney organ culture.
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Other Notes
Tradtrantip, L., et al. 2009. J. Med. Chem.52, 6447.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51282908
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 219677-10MG
