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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model.
Tradtrantip L, et al. J Med Chem. 2009 Oct 22;52(20):6447-55. PMID: 19785436.
|Related CFTR Products|
GLPG1837 (ABBV-974) is a novel CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
VX-661 is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface.
IOWH032 is a synthetic CFTR inhibitor with IC50 of 1.01 μM in CHO-CFTR cell based assays. Phase 1/2.
CFTRinh-172 is a voltage-independent, selective CFTR inhibitor with Ki of 300 nM, showing no effects on MDR1, ATP-sensitive K+ channels, or a series of other transporters.
VX-809 is a CFTR corrector that improves CFTR processing and maturation in the cell.
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