A-803467

A-803467 - Names and Identifiers

Name	5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide
Synonyms	A-803467 A 803467 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)- 5-(4-Chlorophenyl)-furan-2-carboxylic acid 3,5 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)-2-furancarboxamide 5-4(-Chlorophenyl)-N-(3,5-diMethoxyphenyl)furan-2-carboxaMide 5-(4-chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide 2-FurancarboxaMide,5-(4-chlorophenyl)-N-(3,5-diMethoxyphenyl)- 5-(4-Chlorophenyl)-furan-2-carboxylic acid 3,5-dimethoxyphenylamide
CAS	944261-79-4

A-803467 - Physico-chemical Properties

Molecular Formula	C19H16ClNO4
Molar Mass	357.79
Density	1.294±0.06 g/cm3(Predicted)
Melting Point	128-130?C
Boling Point	450.6±45.0 °C(Predicted)
Solubility	DMSO: >10mg/mL
Appearance	powder
Color	white to tan
pKa	11.72±0.70(Predicted)
Storage Condition	room temp
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.
MDL	MFCD10574689
Use	A-803467
In vitro study	A- 803467 effectively blocked the recombinant human or rat Nav1.8 channel with an IC50 of 8 nM and 45 nM, respectively, maintaining A potential of -40 mV. At the resting potential, A- 803467 also effectively blocks the human Nav1.8 pathway with an IC50 of 79 nM. A- 803467 blocked the current of anti-Tetrodotoxin(TTX-R) in rat dorsal root ganglion neurons in A concentration-dependent manner, with an IC50 of 140 nM, which was higher than that of Mexiletine and Lamotrigine(IC50>30 μm). More effective. A- 803467 was 300 to 1000-fold more selective for hNav1.8 than hNav1.2, hNav1.3, hNav1.5, and hNav1.7 channels, with IC50 values of 7.38 μm, 2.45 μm, and 7.34 μm, respectively, and 6.74 μm. A- 803467 acts on peripheral sensory neuron channels and receptors, including TRPV1, P2X2/3, Cav2.2 and KCNQ2/3 channels, with no significant activity, IC50>10 μm. A- 803467 of 0.3 μm, but not 0.1 μm, Significantly Inhibited Spontaneous and electrically stimulated evoked action potential production. A- 803467 effectively blocked recombinant human or rat Na v 1.8 channels with an IC50 of 8 nM and 45 nM, respectively, maintaining A potential of -40 mV. At the resting potential, A- 803467 also effectively blocks the human Na v 1.8 pathway, The IC50 was 79 nM. A- 803467 blocked the current of anti-Tetrodotoxin(TTX-R) in rat dorsal root ganglion neurons in A concentration-dependent manner, with an IC50 of 140 nM, which was higher than that of Mexiletine and Lamotrigine(IC50>30 μm). More effective. The channel selectivity of A- 803467 for hNa v 1.8 is 1.2-to 1.3-fold higher than that for hNa v 1.5, hNa v 1.7, hNa v 300, and hNa v 1000, with an IC50 of 7.38 μm, 2.45 M, 7.34 M, and 6.74 M. A- 803467 acts on peripheral sensory neuron channels and receptors, including TRPV1, P2X 2/3, Ca v 2.2 and KCNQ2/3 channels, with no significant activity, IC50>10 μm. A- 803467 of 0.3 μm, but not 0.1 μm, Significantly Inhibited Spontaneous and electrically stimulated evoked action potential production.
In vivo study	Consistent with the in vitro effect on neuronal action potential electrogenesis, A- 803467 spinal nerve ligation rats were intravenously administered at a dose of 20 mg/kg, spontaneous and von Frey hair-induced wide dynamic range neurons in the spinal dorsal horn were significantly reduced by 66% and 53%, respectively. A- 803467 acts on A variety of rat pain models, including spinal nerve ligation (ED50=47 mg/kg, intraperitoneal injection), sciatic nerve injury (ED50=85 mg/kg, intraperitoneal injection), secondary mechanical allodynia induced by capsaicin (ED50 ≈ 100 mg/kg, I. P.) and thermal hyperalgesia induced by complete plantar injection of Freund's adjuvant (ED50=41 mg/kg, intraperitoneal injection), also reduce mechanical pain, this effect is dose dependent. A- 803467 had no activity on formalin-induced injury and acute heat and post-operative pain, as well as on the chemotherapy-induced pain model (Vincristine). consistent with the electrogenesis of action potential of neurons in vitro, A- 803467 spinal nerve ligation rats were intravenously injected at a dose of 20 mg/kg, spontaneous and von Frey hair-induced wide dynamic range neurons in the spinal dorsal horn were significantly reduced by 66% and 53%, respectively. A- 803467 acts on A variety of rat pain models, including spinal nerve ligation (ED50=47 mg/kg, intraperitoneal injection), sciatic nerve injury (ED50=85 mg/kg, intraperitoneal injection), secondary mechanical allodynia induced by capsaicin (ED50 ≈ 100 mg/kg, I. P.) and thermal hyperalgesia induced by complete plantar injection of Freund's adjuvant (ED50=41 mg/kg, intraperitoneal injection), also reduce mechanical pain, this effect is dose dependent. A- 803467 had no activity on formalin-induced injury and acute heat and post-operative pain, as well as on the chemotherapy-induced pain model (Vincristine).