A-803467

Product details

• Chemical name: 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide.
• CAS number: 944261-79-4
• Molecular formula: C19H16ClNO4.
• Purity: >99% (HPLC)
• Concentration: 10 nM - 10 μM.
• Form: Lyophilized Powder
• Solubility: DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Shipping: 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.
• Target: NaV1.8 Na+ channels
• Source: Synthetic
• Activity: A-803467 is a potent and selective blocker of the TTX-resistant NaV1.8 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 states1,2. 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 heart3.

Scientific background

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 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 NaV1.8 channel might serve as a target in pain control2-4.A-803467 is a potent and selective blocker of the TTX-resistant NaV1.8 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 states4,5. 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 heart6.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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