Description: Potent and selective NaV1.8 channel blocker; active in vivo
Chemical Name: 1-Methyl-[1-[4-(4-trifluoromethoxy)phenyl]-imidazol-2-yl]-ethanamine
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Bagalet 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: