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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related CFTR Products |
|---|
| 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). |
| (R)-Olacaftor
(R)-Olacaftor is a cystic fibrosis transmembrane regulator (CFTR) modulator that can be used in cystic fibrosis (CF) related studies. |
| CFTR corrector 9
CFTR corrector 9 is a cystic fibrosis transmembrane conductance regulator protein (CFTR) modulator for cystic fibrosis (CF) and other CFTR-related diseases. |
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