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PPQ-102

Cat. No. M3147

PPQ-102 Structure
Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 270 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 438.48
Formula C26H22N4O3
CAS Number 931706-15-9
Purity >99%
Solubility DMSO
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PPQ-102 supplier, CFTR, inhibitors

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