Cat. No. 2976
Chemical Name: 5-(4-Chlorophenyl)-N-(3,5-dimethoxy
Biological ActivitySelective blocker of NaV1.8 channels (IC50 values are 8, 2450, 6740, 7340 and 7380 nM for hNaV1.8, hNaV1.3, hNaV1.7, hNaV1.5 and hNaV1.2 channels respectively). Shows no significant activity against TRPV1, P2X2/3, CaV2.2 and KCNQ2/3 channels. Antinociceptive; potently attenuates mechanical allodynia in two models of neuropathic pain following i.p. administration.
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Kort et al (2008) 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. J.Med.Chem. 51 407. PMID: 18176998.
McGaraughty et al (2008) 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. J.Pharmacol.Exp.Ther. 324 1204. PMID: 18089840.
Jarvis et al (2007) A-803467, a potent and selective NaV1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc.Natl.Acad.Sci. 104 8520.
Rush and Cummins (2007) Painful research: identification of a small-molecule inhibitor that selectively targets NaV1.8 sodium channels. Mol.Interv. 7 192. PMID: 17827438.
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Citations are publications that use Tocris products. Selected citations for A 803467 include:
Wu et al (2016) CXCL13/CXCR5 enhances sodium channel Nav1.8 current density via p38 MAP kinase in primary sensory neurons following inflammatory pain Scientific Reports 6 34836. PMID: 27708397.
Curtright et al (2015) Modeling nociception in zebrafish: a way forward for unbiased analgesic discovery. PLoS One 10 e0116766. PMID: 25587718.
Mascanfroni et al (2015) Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α. Biol Open 21 638. PMID: 26005855.
Stone et al (2013) Attenuation of autonomic reflexes by A803467 may not be solely caused by blockade of NaV 1.8 channels. Nat Med 543 177. PMID: 23523647.
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Keywords: A 803467, supplier, Selective, NaV18, blockers, Sodium, Channels, voltage-gated, voltage-dependent, Na+, A803467, Tocris Bioscience, Voltage-gated Sodium (NaV) Channel Blocker products