A3109
A-803467
≥98% (HPLC), Nav1.8 sodium channel blocker, powder
Synonym(s):
5-4(-Chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide
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About This Item
Empirical Formula (Hill Notation):
C19H16NO4Cl
CAS Number:
Molecular Weight:
357.79
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Product Name
A-803467, ≥98% (HPLC)
Quality Level
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
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.
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Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads (2017)
Mihai Moldovan et al.
Neurobiology of aging, 39, 128-139 (2016-03-01)
Accumulating myelin abnormalities and conduction slowing occur in peripheral nerves during aging. In mice deficient of myelin protein P0, severe peripheral nervous system myelin damage is associated with ectopic expression of Nav1.8 voltage-gated Na(+) channels on motor axons aggravating the
Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad (2010)