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A 803467

Selective NaV1.8 channel blocker

Product Code: Asc-282

Purity: >98%

 
Pack Size

 

10mg

50mg

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Biological Description

Selective blocker of NaV1.8 channels (IC50 = 8 nM for human NaV1.8 ). Shows greater than 100-fold selectivity over human NaV1.2, NaV1.3, NaV1.5, and NaV1.7 (IC50 values ?1 ?M). Shows no significant activity against TRPV1, P2X2/3, CaV2.2 and KCNQ2/3 channels. Antinociceptive.

Useful References

(2007) A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci U S A. 104:8520-5. abstract

(2007) Painful research: identification of a small-molecule inhibitor that selectively targets Nav1.8 sodium channels. Mol Interv. 7:192-5 abstract

(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. 324:1204-11. abstract

Citations

Effective contractile effect of voltage-gated Na+ channels revealed by a channel activator. abstract

Chemical Information

5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide

Asc-282
  • Desiccate at RT
  • MW 357.79
  • Soluble in DMSO to 100 mM and in ethanol to 25 mM
  • C19H16ClNO4
  • 944261-79-4