A sodium channel blocker with high-affinity and selectivity for inhibiting human Nav1.8 sodium channels (IC50 = 8 nM when stimulated at half-maximal inactivation and IC50 = 79 nM at a resting state); dose dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models

A-803467 – 10 mg

Brand:
Cayman
CAS:
944261-79-4
Storage:
-20
UN-No:
Non-Hazardous - /

Nav1.8 is a tetrodotoxin-resistant (TTX-R) sodium channel with high activation threshold and slow inactivating kinetics that is highly expressed in small-diameter sensory neurons and has been implicated in signaling various types of pain. A-803467 is a sodium channel blocker with high-affinity and selectivity for inhibiting human Nav1.8 sodium channels (IC50 = 8 nM when stimulated at half-maximal inactivation and IC50 = 79 nM at a resting state). {16698} This compound is unusual in that it blocks hNav1.8 at negative resting membrane potentials (many small molecule sodium channel blockers show a reduced affinity for the resting state) and does not demonstrate significant frequency-dependent block during a 10 Hz pulse train.{16697} A-803467 dose-dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models.{16698}  

 

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Description

A sodium channel blocker with high-affinity and selectivity for inhibiting human Nav1.8 sodium channels (IC50 = 8 nM when stimulated at half-maximal inactivation and IC50 = 79 nM at a resting state); dose dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models

Formal name: 5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide

Synonyms: 

Molecular weight: 357.8

CAS: 944261-79-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Neuroscience|Pain Research

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