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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

A-803467

Cayman Chemical Item Number 10012588

(CAS 944261-79-4)

A-803467 (CAS 944261-79-4)

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Description

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).1 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.2 A-803467 dose-dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models.1

1 Jarvis, M.F., Honore, P., Shieh, C., et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci USA 104(20) 8520-8525 (2007).

2 Krafte, D.S., Chapman, M., Marron, B., et al. Block of NAv1.8 by small molecules. Channels 1(3) 152-153 (2007).

Formal Name 5-​(4-​chlorophenyl)-​N-​(3,​5-​dimethoxyphenyl)-​2-​furancarboxamide
CAS Number 944261-79-4
Molecular Formula C19H16ClNO4
Formula Weight 357.8
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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COc1cc(OC)​cc(c1)​NC(=O)​c1ccc(o1)​c1ccc(Cl)​cc1

Background Reading

Jarvis, M.F., Honore, P., Shieh, C., et al. A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. Proc Natl Acad Sci USA 104(20) 8520-8525 (2007).

Krafte, D.S., Chapman, M., Marron, B., et al. Block of NAv1.8 by small molecules. Channels 1(3) 152-153 (2007).
Size Price Quantity Subtotal
5 mg $29.00 $0.00
10 mg $55.00 $0.00
50 mg $232.00 $0.00
100 mg $406.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-02-12. Prices are subject to change without notice.

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