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A3109

A-803467

Name: A-803467
Brand: SIGMA

≥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:

944261-79-4

Molecular Weight:

357.79

UNSPSC Code:

12352200

PubChem Substance ID:

329770815

NACRES:

NA.77

MDL number:

MFCD10574689

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Product Name

A-803467, ≥98% (HPLC)

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

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Bioactive Small Molecules

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 IC₅₀of 8 nM and IC₅₀of 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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number

0000426823

0000382440

0000261924

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Aging-associated changes in motor axon voltage-gated Na(+) channel function in mice.

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

Painful research: identification of a small-molecule inhibitor that selectively targets Nav1.8 sodium channels.

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

Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad (2010)

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Journal of thrombosis and haemostasis : JTH, 15(6), 1223-1235 (2017-03-28)

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Articles

Sodium Channels

Voltage-gated sodium channels are present in most excitable cell membranes and play an important role in generating action potentials.

钠通道

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。

Global Trade Item Number

SKU	GTIN
A3109-50MG	04061832569079
A3109-10MG	04061832569062

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