Chemical Name: 1-Methyl-[1-[4-(4-trifluoromethoxy)phenyl]-imidazol-2-yl]-ethanamine
Biological ActivityPotent 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.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of selective NaV1.8 modulators for the treatment of chronic pain. Abstract.
Bagal et al.
4th RSC/SCI Symp. on Ion Channels as Ther. Targ, 2013;
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PF 04885614 as an inhibitor was used to understand the modulation of peripheral sensitisation.