Purity >95%. The cystic fibrosis (CF) gene encodes a cAMP-regulated chloride channel, the CF transmembrane conductance regulator (CFTR). PPQ-102 is a cell-permeable pyrimido-pyrrolo-quinoxalinedione that reversibly inhibits CFTR chloride channels with an IC50 value of 90 nM. At 0.5-5 μM, PPQ-102 has been used to reduce the size and number of renal cysts in a neonatal kidney organ culture model of polycystic kidney disease. At 1 μM, PPQ-102 can increase vascular endothelial growth factor-A production in cultured airway epithelial NCI-H292 cells, triggering epidermal growth factor receptor phosphorylation.
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Other Names
6,7-dihydro-7,9-dimethyl-6-(5-methyl-2-furanyl)-11-phenyl-pyrimido[4',5':3,4]pyrrolo[1,2-a]quinoxaline-8,10(5H,9)-dione, CFTR Inhibitor IV, Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV