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PPQ-102

Cat. No. M3147
PPQ-102 Structure
Synonym:

CFTR Inhibitor

Size Price Availability Quantity
10mM*1mL in DMSO USD 110  USD110 In stock
5mg USD 100  USD100 In stock
10mg USD 170  USD170 In stock
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Tradtrantip L, et al. J Med Chem. Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model.

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  Catalog
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Keywords: PPQ-102, CFTR Inhibitor supplier, CFTR, inhibitors, activators


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