A 803467
Chemical Name: 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide
Purity: ≥98%
Biological Activity
A 803467 is a selective blocker of Na V 1.8 channels (IC 50 values are 8, 2450, 6740, 7340 and 7380 nM for hNa V 1.8, hNa V 1.3, hNa V 1.7, hNa V 1.5 and hNa V 1.2 channels respectively). Shows no significant activity against TRPV1, P2X 2/3 Ca V 2.2 and KCNQ2/3 channels. Antinociceptive; potently attenuates mechanical allodynia in two models of neuropathic pain following i.p. administration.Technical Data
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.
Background References
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Painful research: identification of a small-molecule inhibitor that selectively targets NaV1.8 sodium channels.
Rush and Cummins
Mol.Interv., 2007;7:192 -
A selective NaV1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats.
McGaraughty et al.
J.Pharmacol.Exp.Ther., 2008;324:1204 -
Discovery and biological evaluation of 5-Aryl-2-furfuramides, potent and selective blockers of the Nav1.8 sodium channel with efficacy in models of neuropathic and inflammatory pain.
Kort et al.
J.Med.Chem., 2008;51:407
Product Datasheets
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Citations for A 803467
The citations listed below are publications that use Tocris products. Selected citations for A 803467 include:
7 Citations: Showing 1 - 7
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CXCL13/CXCR5 enhances sodium channel Nav1.8 current density via p38 MAP kinase in primary sensory neurons following inflammatory pain
Authors: Wu Et al.
Scientific Reports 2016;6:34836
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Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α.
Authors: Mascanfroni Et al.
Biol Open 2015;21:638
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Modeling nociception in zebrafish: a way forward for unbiased analgesic discovery.
Authors: Curtright Et al.
PLoS One 2015;10:e0116766
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Functional upregulation of nav1.8 sodium channels on the membrane of dorsal root Ganglia neurons contributes to the development of cancer-induced bone pain.
Authors: Liu Et al.
PLoS One 2014;9:e114623
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Attenuation of autonomic reflexes by A803467 may not be solely caused by blockade of NaV 1.8 channels.
Authors: Stone Et al.
Nat Med 2013;543:177
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Common mechanisms of drug interactions with sodium and T-type calcium channels.
Authors: Bladen
Mol Pharmacol 2012;82:481
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Involvement of Nav 1.8 sodium ion channels in the transduction of mechanical pain in a rodent model of osteoarthritis.
Authors: Schuelert and McDougall
Arthritis Res Ther 2012;14:R5
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