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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Articles
Voltage-gated sodium channels are present in most excitable cell membranes and play an important role in generating action potentials.
电压门控钠通道存在于大多数可兴奋细胞膜中，在产生动作电位方面起着重要作用。
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
Anthony M Rush et al.
Molecular interventions, 7(4), 192-195 (2007-09-11)
Voltage-gated sodium channels in nociceptive neurons are attractive targets for novel pain therapeutics. Although drugs that target voltage-gated sodium channels have proven value as pain therapeutics, the drugs that are currently available are non-specific sodium channel inhibitors, which limit their
Global Trade Item Number
| SKU | GTIN |
|---|---|
| A3109-50MG | 04061832569079 |
| A3109-10MG | 04061832569062 |