A-803467 (C005B-091083)

General description

A-803467 inhibits spontaneous and evoked action potentials in sensory neurons. It exhibits antinociceptive effects. A-803467 decreases the firing in spinal dorsal horn neurons in vivo.

The small molecule A-803467 is a potent and selective Nav1.8 sodium channel blocker. Nav1.8 is a tetrodotoxin-resistant (TTX-R) sodium channel that contributes to pain sensation by transmitting pain stimuli in peripheral sensory neurons; blockage of this channel by A-803467 reduces pain with varying effectiveness in a number of different models. A-803467 has been used to further understand the role of Nav1.8 in transmitting pain stimuli and also can be used as an analgesic.

Biochem/physiol Actions

A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC₅₀ of 8 nM and IC₅₀ of 79 nM, respectively. A-803467 is over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7.

Features and Benefits

This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Molecular Weight: 357.79. Empirical Formula: C₁₉H₁₆NO₄Cl. Quality Level: 100. Assay: ≥. 98% (HPLC). form: powder. color: white to tan. solubility: DMSO: >. 10 . mg/mL. originator: Abbott. storage temp.: room temp. SMILES string: COc1cc(NC(: O)c2ccc(o2)-c3ccc(Cl)cc3)cc(OC)c1. InChI: 1S/C19H16ClNO4/c1-23-15-9-14(10-16(11-15)24-2)21-19(22)18-8-7-17(25-18)12-3-5-13(20)6-4-12/h3-11H,1-2H3,(H,21,22). InChI key: VHKBTPQDHDSBSP-UHFFFAOYSA-N. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.