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| 5-(4-Chlorophenyl)-furan-2-carboxylic acid 3,5-dimethoxyphenylamide Basic information |
| 5-(4-Chlorophenyl)-furan-2-carboxylic acid 3,5-dimethoxyphenylamide Chemical Properties |
| Melting point | 128-130?C | | Boiling point | 450.6±45.0 °C(Predicted) | | density | 1.294±0.06 g/cm3(Predicted) | | storage temp. | room temp | | solubility | DMSO: >10mg/mL | | form | powder | | pka | 11.72±0.70(Predicted) | | color | white to tan | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Hazard Codes | Xn | | Risk Statements | 22 | | WGK Germany | 3 |
| 5-(4-Chlorophenyl)-furan-2-carboxylic acid 3,5-dimethoxyphenylamide Usage And Synthesis |
| 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). 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. A-803467 dose-dependently reduces behavioral responses in a variety of neuropathic and inflammatory pain models. | | Chemical Properties | White Solid | | Uses | A selective NaV1.8 sodium channel blocker, reduces behavioral measures of chronic pain. | | Uses | A selective NaV1.8 sodium channel blocker, reduces behavioral measures of chronic pain. Analgesic. | | General Description | The small molecule A-803467 is a potent and selective Nav1.8 sodium channel blocker. Nav1.8 is a tetrodotoxin-resistant (TTX-R) sodium channel that contributes to pain sensation by transmitting pain stimuli in peripheral sensory neurons; blockage of this channel by A-803467 reduces pain with varying effectiveness in a number of different models. A-803467 has been used to further understand the role of Nav1.8 in transmitting pain stimuli and also can be used as an analgesic. | | Biological Activity | Selective blocker of Na V 1.8 channels (IC 50 values are 8, 2450, 6740, 7340 and 7380 nM for hNa V 1.8, hNa V 1.3, hNa V 1.7, hNa V 1.5 and hNa V 1.2 channels respectively). Shows no significant activity against TRPV1, P2X 2/3 , Ca V 2.2 and KCNQ2/3 channels. Antinociceptive; potently attenuates mechanical allodynia in two models of neuropathic pain following i.p. administration. | | Biochem/physiol Actions | A-803467 blocks Nav1.8 in both half-maximal inactive and resting states with an IC50 of 8 nM and IC50 of 79 nM, respectively. A-803467 is over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7. | | References | 1) Jarvis et al. (2007), 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 8520
2) McGaraughty et al. (2008), A selective Nav1.8 sodium channel blocker, A-803467 [5-(4-chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], attenuates spinal neuronal activity in neuropathic rats; J. Pharmacol. Exp. Ther., 324 1204 |
| 5-(4-Chlorophenyl)-furan-2-carboxylic acid 3,5-dimethoxyphenylamide Preparation Products And Raw materials |
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