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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.
Sold for research purposes under agreement from Pfizer Inc.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 the degree 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|
References are publications that support the biological activity of the product.
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
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Citations for PF 04885614
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Literature in this Area
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.