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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
A-803467 is a potent and selective blocker of Nav1.8 sodium channel with IC50 value of 8nM [1].
A-803467 is a sodium channel blocker with high affinity and selectivity. It blocks the human Nav1.8 channels with IC50 value of 79nM. It also blocks the recombinant rat Nav1.8 channels with IC50 value of 45nM when the holding potential is -40mV. A-803467 is highly selective against Nav1.8 since the inhibition of Nav1.8 is 300- to 1000-fold more potent than of NaV1.2, NaV1.3, NaV1.5, and NaV1.7. It is found that A-803467 effectively suppresses the evoked and spontaneous action potential firing in DRG neurons in which TTX-R currents play a remarkable role. Furthermore, the selective blockade of Nav1.8 channels results in a significant reduction in nociceptive sensitivity. A-803467 potently attenuates mechanical allodynia in models of neuropathic pain. It also potently reduces thermal hyperalgesia in the CFA model of inflammatory pain [1].
References:[1] Jarvis M F, Honore P, Shieh C C, et al. A-803467, a potent and selective Nav1. 8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proceedings of the National Academy of Sciences, 2007, 104(20): 8520-8525.
Cell lines
Rat dorsal root ganglion (DRG) neurons and HEK-293 cells expressing human Nav1.8 sodium channels
Preparation method
The solubility of this compound in DMSO is > 13.95 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.
Reacting condition
0 ~ 100 μM
Applications
A-803467 at the dose of 100 nM significantly blocks recombinant human and native rat Nav1.8 currents. In rat DRG neurons, A-803467 concentration-dependently blocked tetrodotoxin-resistant (TTX-R) current at the potential of -40 mV, with the IC50 value of 140 nM.
Animal models
Spinal nerve ligated rats
Dosage form
20 mg/kg; i.v.
In spinal nerve ligated rats, A-803467 markedly reduced spontaneous and von Frey hair evoked firing of spinal dorsal horn wide dynamic range neurons by 66% and 53%, respectively, which implied that systemic administration of A-803467 altered the activity of spinal sensory neurons. In addition, these effects of A-803467 were dose-dependent.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1]. Jarvis M F, Honore P, Shieh C C, et al. A-803467, a potent and selective Nav1. 8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proceedings of the National Academy of Sciences, 2007, 104(20): 8520-8525.