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Merck
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Documentos

A3109

Sigma-Aldrich

A-803467

≥98% (HPLC)

Sinónimos:

5-4(-Chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide

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About This Item

Fórmula empírica (notación de Hill):
C19H16NO4Cl
Número de CAS:
944261-79-4
Peso molecular:
357.79
MDL number:
MFCD10574689
UNSPSC Code:
12352200
PubChem Substance ID:
329770815
NACRES:
NA.77

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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DNQX ≥98% (TLC)

Sigma-Aldrich

D0540

DNQX

K Bekő et al.
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Essentials The role of platelet P2Y Background P2Y
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
Peripheral Receptor Targets for Analgesia: Novel Approaches to Pain Management (2009)
Enzyme Inhibition in Drug Discovery and Development: The Good and the Bad (2010)
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
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Sodium Channels

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

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