Biological Activity
Potent, voltage-independent CFTR chloride channel inhibitor (IC50 = 90 nM). Reduces the size and number of renal cysts in an embryonic kidney culture model of polycystic kidney disease. Also increases VEGF-A production from airway epithelial cells in vitro.
Technical Data
| M. Wt | 438.48 |
| Formula | C26H22N4O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 931706-15-9 |
| PubChem ID | 16016583 |
| InChI Key | MNOOVRNGPIWJDI-UHFFFAOYSA-N |
| Smiles | O=C(N2C)C1=C(C3=CC=CC=C3)N4C(C(C6=CC=C(C)O6)NC5=C4C=CC=C5)=C1N(C)C2=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 8.77 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 438.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.28 mL | 11.4 mL | 22.81 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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References
References are publications that support the products' biological activity.
Tradtrantip et al (2009) Nanomolar potency pyrimido-pyrrolo-quinoxalinedione CFTR inhibitor reduces cyst size in a polycystic kidney disease model. J.Med.Chem. 52 6447 PMID: 19785436
Martin et al (2013) CFTR dysfunction induces vascular endothelial growth factor synthesis in airway epithelium. Eur.Resp.J. 42 1553 PMID: 23520314
Keywords: PPQ 102, supplier, PPQ102, potent, voltage, independent, CFTR, chloride, channel, inhibitors, inhibits, cystic, fibrosis, transmembrane, conductance, CFTR, CFTR, Tocris Bioscience
