A-803467 potently blocks recombinant human or rat NaV1.8 channels with IC50 of 8 nM and 45 nM, respectively, at a holding potential of -40 mV. At a resting state, A-803467 also potently blocks human NaV1.8 channels with IC50 of 79 nM. A-803467 blocks tetrodotoxin-resistant (TTX-R) currents in rat dorsal root ganglion neurons in a concentration-dependent manner with IC50 of 140 nM, more potently compared with both mexiletine and lamotrigine with IC50 of >30 ¦ÌM. A-803467 displays 300- to 1,000-fold higher selectivity for hNaV1.8 over hNaV1.2, hNaV1.3, hNaV1.5, and hNaV1.7 channels with IC50 of 7.38 ¦ÌM, 2.45 ¦ÌM, 7.34 ¦ÌM, and 6.74 ¦ÌM, respectively. A-803467 shows no significant activity against other channels and receptors expressed in peripheral sensory neurons including TRPV1, P2X2/3, CaV2.2 and KCNQ2/3 channels with IC50 >10 ¦ÌM. A-803467 also shows no or weak activity against a broad screening panel of cell-surface receptors, ion channels, and enzymes with IC50 of >2 ¦ÌM. A-803467 at 0.3 ¦ÌM but not 0.1 ¦ÌM significantly inhibits the generation of spontaneous and electrically evoked action potentials. [

June 21, 2017

prudect name : A-803467 potently blocks recombinant human or rat NaV1.8 channels with IC50 of 8 nM and 45 nM, respectively, at a holding potential of -40 mV. At a resting state, A-803467 also potently blocks human NaV1.8 channels with IC50 of 79 nM. A-803467 blocks tetrodotoxin-resistant (TTX-R) currents in rat dorsal root ganglion neurons in a concentration-dependent manner with IC50 of 140 nM, more potently compared with both mexiletine and lamotrigine with IC50 of >30 ¦ÌM. A-803467 displays 300- to 1,000-fold higher selectivity for hNaV1.8 over hNaV1.2, hNaV1.3, hNaV1.5, and hNaV1.7 channels with IC50 of 7.38 ¦ÌM, 2.45 ¦ÌM, 7.34 ¦ÌM, and 6.74 ¦ÌM, respectively. A-803467 shows no significant activity against other channels and receptors expressed in peripheral sensory neurons including TRPV1, P2X2/3, CaV2.2 and KCNQ2/3 channels with IC50 >10 ¦ÌM. A-803467 also shows no or weak activity against a broad screening panel of cell-surface receptors, ion channels, and enzymes with IC50 of >2 ¦ÌM. A-803467 at 0.3 ¦ÌM but not 0.1 ¦ÌM significantly inhibits the generation of spontaneous and electrically evoked action potentials. [
A-803467

Synonyms: CAS NO: 944261-79-4Molecular Formula: C19H16ClNO4Molecular Weight: 357.79Purity: 98% minSolubility: In DMSOStorage: -20°C


1453848-26-4 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18496984