Biological descriptionSelective 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 μM). Shows no significant activity against TRPV1, P2X2/3, CaV2.2 and KCNQ2/3 channels. Antinociceptive.
Storage instructionsStore at Room Temperature. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 100 mM and in ethanol to 25 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
McGaraughty S et al. 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 Ther324:1204-11 (2008).
Read more (PubMed: 18089840) »
Jarvis MF et al. 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 A104:8520-5 (2007).
Read more (PubMed: 17483457) »
Rush AM & Cummins TR Painful research: identification of a small-molecule inhibitor that selectively targets Nav1.8 sodium channels. Mol Interv7:192-5, 180 (2007).
Read more (PubMed: 17827438) »