Supplier:
Alomone Labs Ltd.Cat no: A-105
A-803467
The TTX-resistant, Nav1.8 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 potentials. Hyperexcitability, manifested by increased action potential firing and coded information transfer to the CNSпїЅof nociceptive DRG neurons, probably lie on the basis of several pathological pain states. Both genetic and pharmacological evidence suggest that Nav1.8 channel might serve as a target in pain control.
A-803467 is a potent and selective blocker of the TTX-resistant Nav1.8 channels. A-803467 is a state dependent inhibitor of the channel, 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.
A-803467, was used as a pharmacological tool to demonstrate the expression of Nav1.8 in the heart conduction system and its contribution to QRS interval in the mouse heart.
Ion Channel Modulators; Voltage - Gated Na+ Channel Blockers.
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SPECIFICATIONS
Catalog Number
A-105
Size
25 mg
Purity
>99%
Concentration
10 nM - 10 uM
Shipping Temp
Room Temperature
Molecular Weight
357.8 da
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