Name: A-803467
Brand: Alomone Labs
SKU: A-105

Overview

Cat #: A-105

Lyophilized Powder yes

Source Synthetic

MW: 357.8

Purity: >99% (HPLC)

Effective concentration 10 nM - 10 μM.

Structure

Chemical name 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide.

Molecular formula C₁₉H₁₆ClNO₄.

CAS No.: 944261-79-4

Activity A-803467 is a potent and selective blocker of the TTX-resistant Na_V1.8 channel. A-803467 is a state dependent inhibitor with IC₅₀ of 8 nM at depolarized membrane potential (-40 mV) and 80 nM at -100 mV. As an efficient inhibitor of TTX-resistant currents in DRG neurons, A-803467 was also effective as an analgesic in several rodent models of different pathological pain states^1,2. A-803467 was used as a pharmacological tool to demonstrate the expression of Na_V1.8 in the heart conduction system and its contribution to QRS interval in the mouse heart³.

References-Activity

Jarvis, M.F. et al. (2007) Proc. Natl. Acad. Sci. U.S.A. 104, 8520.
McGaraughty, S. et al. (2008) J.Pharmacol. Exp. Ther. 324, 1204.
Sotoodehnia, N. et al. (2010) Nat. Gen. 42, 1068.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Our bioassay

Alomone Labs A-803467 inhibits Na_V1.8 channels stably transfected in ND7/23 cells.
Currents were elicited by 50 ms voltage ramp from the holding potential of -100 mV to +60 mV, applied every 10 sec, using whole-cell voltage clamp technique. A. Time course of Na_V1.8 current amplitude changes as a result of A-803467 (#A-105) application at increasing concentrations, as indicated by the horizontal bars. B. Superimposed traces of Na_V1.8 currents under control conditions and after 100 sec perfusion with 10^-8-10^-6M A-803467, as indicated.

References - Scientific background

Renganathan, M. et al. (2001) J. Neurophysiol. 86, 629.
Lai, J. et al. (2002) Pain 95, 143.
Zimmermann, K. et al. (2007) Nature 447, 855.
Jarvis, M.F. et al. (2007) Proc. Natl. Acad. Sci. U.S.A. 104, 8520.
McGaraughty, S. et al. (2008) J.Pharmacol. Exp. Ther. 324, 1204.
Sotoodehnia, N. et al. (2010) Nat. Gen. 42, 1068.

Scientific background

The TTX-resistant Na_V1.8 channel is expressed almost exclusively in the PNS and has been shown to mediate most of the well documented TTX-resistant currents of DRG neurons' action potentials¹. Hyperexcitability, manifested by increased action potential firing and coded information transfer to the CNS of nociceptive DRG neurons, probably lie on the basis of several pathological pain states. Both genetic and pharmacological evidence suggest that Na_V1.8 channel might serve as a target in pain control^2-4.

A-803467 is a potent and selective blocker of the TTX-resistant Na_V1.8 channel⁴. A-803467 is a state dependent inhibitor with IC₅₀ 8 nM at depolarized membrane potential (-40 mV) and 80 nM at -100 mV. As an efficient inhibitor of TTX-resistant currents in DRG neurons, A-803467 was also effective as an analgesic in several rodent models of different pathological pain states^4,5. A-803467 was used as a pharmacological tool to demonstrate the expression of Na_V1.8 in the heart conduction system and its contribution to QRS interval in the mouse heart⁶.

Target Na_V1.8 Na⁺ channels

Lyophilized Powder

A-803467 (#A-105) is a highly pure, synthetic, and biologically active compound.

Certificate of Analysis SDS

For research purposes only, not for human use

Last Update: 05/06/2024

Applications

Citations

Product citations

Lu, V.B. et al. (2015) J. Neurosci. 35, 8021.

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A-803467

Overview

Applications

Citations

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Scientific Background

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