Biological Activity
Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator. Corrects gating defects of CFTR mutants such as ΔF508 (Ka = 0.3 μM), E193K and G970R (Kd values are 0.22 μM and 0.45 μM respectively). Increases ΔF508-CFTR Cl- currents in the presence of forskolin; displays no effect on Ca2+-activated Cl- current.
Technical Data
| M. Wt | 439.55 |
| Formula | C28H29N3O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 853138-65-5 |
| PubChem ID | 4695397 |
| InChI Key | PQAYCXMQTUEDRD-UHFFFAOYSA-N |
| Smiles | O=C(C(C2=CC=CC=C2)N(C)C(CC3=CNC4=C3C=CC=C4)=O)NC1=CC=C(C(C)C)C=C1 |
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 | 43.95 | 100 | |
| ethanol | 2.2 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 439.55. 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 | 11.38 mL | 22.75 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.55 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Pedemonte et al (2005) Phenylglycine and sulphonamide correctors of defective DF508 and G551D cystic fibrosis transmembrane conductance regulator chloride-channel gating. Mol.Pharmacol. 67 1797 PMID: 15722457
Caputo et al (2009) Mutation-specific potency and efficacy of cystic fibrosis transmembrane conductance regulator chloride channel potentiators. J.Pharmacol.Exp.Ther. 330 783 PMID: 19491324
Pedemonte et al (2010) Influence of cell background on pharmacological rescue of mutant CFTR. Am.J.Physiol.Cell Physiol 298 C866 PMID: 20053923
Keywords: PG 01, supplier, PG01, CTFR, mutant, potentiators, cystic, fibrosis, transmembrane, conductance, channels, CFTR, chloride, Cl-, pharmacochaperones, CFTR, CFTR, Tocris Bioscience
