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PPQ-102 inhibites CFTR chloride current with IC 50 approximately 90 nM. PPQs are uncharged at physiological pH, so not subject to membrane potential-dependent cellular partitioning or block efficiency. PPQ-102 prevents cyst expansion and reduces the size of preformed cysts in a neonatal kidney organ culture model of polycystic kidney disease. PPQ-102 is the most potent CFTR inhibitor identified to date.
| Molecular Weight | 438.48 |
| Formula | C26H22N4O3 |
| CAS Number | 931706-15-9 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related CFTR Products |
|---|
| GLPG2737
GLPG2737 is a potent CFTR type 2 corrector, and GLPG2737 can be used in combination with a type 1 co-corrector in the study of cystic fibrosis. |
| NJH-2-057
NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a agent used to treat cystic fibrosis that binds ΔF508-CFTR. |
| GLPG2737
GLPG2737 is a novel potent Type 2 corrector of CFTR. GLPG2737 showed high permeability both in MDCKII-MDRI and Caco-2 cells, with low efflux allowing an elevated absorbed fraction FaxFg and a dose proportional increase in exposure in rat from a dose of 5 to 300 mg/kg, despite a low aqueous thermodynamic solubility. |
| UCCF-853
UCCF-853 is a cystic fibrosis transmembrane regulatory protein (CFTR) modulator. |
| (R)-Posenacaftor sodium
(R)-Posenacaftor sodium is the R-enantiomer of Posenacaftor and a cystic fibrosis transmembrane regulatory protein (CFTR) modulator that corrects the folding and transport of CFTR proteins.Posenacaftor is used in studies related to cystic fibrosis (CF). |
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