A 803467

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Cat.No. 2976 - A 803467 | C19H16ClNO4 | CAS No. 944261-79-4
Description: Selective NaV1.8 channel blocker
Chemical Name: 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations (7)
Reviews
Literature

Biological Activity

Selective 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.

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Technical Data

M. Wt 357.79
Formula C19H16ClNO4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 944261-79-4
PubChem ID 16038374
InChI Key VHKBTPQDHDSBSP-UHFFFAOYSA-N
Smiles ClC(C=C2)=CC=C2C1=CC=C(C(NC3=CC(OC)=CC(OC)=C3)=O)O1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 35.78 100
ethanol 8.94 25

Preparing Stock Solutions

The following data is based on the product molecular weight 357.79. 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 2.79 mL 13.97 mL 27.95 mL
5 mM 0.56 mL 2.79 mL 5.59 mL
10 mM 0.28 mL 1.4 mL 2.79 mL
50 mM 0.06 mL 0.28 mL 0.56 mL

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Product Datasheets

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References

References are publications that support the biological activity of the product.

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

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

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

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


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Keywords: A 803467, A 803467 supplier, Selective, NaV18, blockers, Sodium, Channels, voltage-gated, voltage-dependent, Na+, A803467, Voltage-gated, 2976, Tocris Bioscience

7 Citations for A 803467

Citations are publications that use Tocris products. Selected citations for A 803467 include:

Mascanfroni et al (2015) Metabolic control of type 1 regulatory T cell differentiation by AHR and HIF1-α. Biol Open 21 638 PMID: 26005855

Liu et al (2014) Functional upregulation of nav1.8 sodium channels on the membrane of dorsal root Ganglia neurons contributes to the development of cancer-induced bone pain. PLoS One 9 e114623 PMID: 25503076

Curtright et al (2015) Modeling nociception in zebrafish: a way forward for unbiased analgesic discovery. PLoS One 10 e0116766 PMID: 25587718

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

Bladen (2012) Common mechanisms of drug interactions with sodium and T-type calcium channels. Mol Pharmacol 82 481 PMID: 22695716

Schuelert and McDougall (2012) Involvement of Nav 1.8 sodium ion channels in the transduction of mechanical pain in a rodent model of osteoarthritis. Arthritis Res Ther 14 R5 PMID: 22225591

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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