Biological Activity
Potent NaV1.8 inhibitor (IC50 = 53 nM for human NaV1.8 channel). Exhibits selectivity for hNaV1.8 over hNaV1.6, hNaV1.7, hNaV1.1, hNaV1.2 and hNaV1.5 (IC50 values are 4.2, 7.0, 11, 16 and 27 μM respectively). Orally bioavailable.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries
PF 04885614 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 285.26 |
| Formula | C13H14F3N3O |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| PubChem ID | 65459349 |
| InChI Key | AGORGFNWYAUYSU-UHFFFAOYSA-N |
| Smiles | CC(C)(N)C1=NC(C2=CC=C(OC(F)(F)F)C=C2)=CN1 |
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 | 28.53 | 100 | |
| ethanol | 28.53 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 285.26. 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 | 3.51 mL | 17.53 mL | 35.06 mL |
| 5 mM | 0.7 mL | 3.51 mL | 7.01 mL |
| 10 mM | 0.35 mL | 1.75 mL | 3.51 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bagal et al (2013) Discovery of selective NaV1.8 modulators for the treatment of chronic pain. Abstract. 4th RSC/SCI Symp. on Ion Channels as Ther. Targ PMID:
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