A cell-permeable pyrimido-pyrrolo-quinoxalinedione that reversibly inhibits CFTR chloride channels (IC50 = 90 nM); reduces the size and number of renal cysts in a neonatal kidney organ culture model of polycystic kidney disease; increases VEGF-A production in cultured airway epithelial NCI-H292 cells

PPQ-102 – 5 mg

Brand:
Cayman
CAS:
931706-15-9
Storage:
-20
UN-No:
Non-Hazardous - /

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.{29223} 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.{29223} 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.{29224}  

 

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Description

A cell-permeable pyrimido-pyrrolo-quinoxalinedione that reversibly inhibits CFTR chloride channels (IC50 = 90 nM); reduces the size and number of renal cysts in a neonatal kidney organ culture model of polycystic kidney disease; increases VEGF-A production in cultured airway epithelial NCI-H292 cells

Formal name: 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

Synonyms:  CFTR Inhibitor IV|Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor IV

Molecular weight: 438.5

CAS: 931706-15-9

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors

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