Fluoxakalner
Fluoxakalner is a selective Kv7.2/7.3 channel opener with an EC50 of 0.36 μM. Fluoxakalner accelerates the activation kinetics of Kv7.2/7.3 channels and produces anti-nociceptive effects. Fluoxakalner is applicable for pain research.
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- Fòrmula: C23H22FNO2
- Peso molecular:363.42
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Kv7.2/7.3 0.36 μM (EC50) |
KV7.2 0.83 μM (EC50) |
KV7.4 3.61 μM (EC50) |
KV7.5 1.23 μM (EC50) |
Fluoxakalner (0.03-10 μM) potently activates Kv7.2/7.3 channels stably expressed in HEK293 cells with an EC50 of 0.36 μM, shifts channel activation to more hyperpolarized potentials, accelerates activation kinetics, and slows deactivation kinetics[1].
Fluoxakalner (0.03-30 μM) preferentially activates Kv7.2/7.3 channels over other Kv7 subtypes, with no activity on Kv7.1 channels, and activates homotetrameric Kv7.2, Kv7.4, and Kv7.5 channels with EC50 values of 0.83 μM, 3.61 μM, and 1.23 μM, respectively, in transfected HEK293/HEK293T cells[1].
Fluoxakalner (10 μM) does not inhibit hERG or Nav1.5 channels stably expressed in CHO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fluoxakalner (1-5 mg/kg; i.p.; single dose) reduces visceral nociceptive behavior in mice, with the 5 mg/kg dose producing a 41% reduction in Acetic acid (HY-Y0319)-induced abdominal writhes[1].
Fluoxakalner (1-5 mg/kg; i.p.; single dose) exerts dose-dependent antinociceptive effects in a mouse acute thermal pain model, with the 5 mg/kg dose increasing tail-flick latency by 50% at 1 h post-administration[1].
Fluoxakalner (1-5 mg/kg; i.p.; single dose) attenuates both acute and inflammatory pain components in the mouse formalin test, with the 5 mg/kg dose yielding significant reductions in nociceptive licking behavior in both test phases[1].
Fluoxakalner (1-10 mg/kg; i.p.; single dose) does not impair locomotor activity or motor coordination in mice at doses up to 10 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 6 weeks old, 18-25 g, CFA-induced inflammatory pain model)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:i.p.; single dose
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Result:Increased PWMT from a baseline of 0.29 g to 0.65 g at 1 h post-administration at 1 mg/kg.
Increased PWTL from a baseline of 6.38 s to 9.82 s at 1 h post-administration at 1 mg/kg.
Increased PWMT from a baseline of 0.29 g to 0.94 g at 1 h post-administration at 5 mg/kg.
Increased PWTL from a baseline of 6.85 s to 11.48 s at 1 h post-administration at 5 mg/kg.
Sustained significant effects on PWMT and PWTL through 4 h post-administration relative to vehicle controls at 5 mg/kg.
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Animal Model:C57BL/6J (male, 6 weeks old, 18-25 g, acetic acid-induced visceral pain model)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:i.p.; single dose
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Result:Reduced the number of abdominal writhes by approximately 30% relative to vehicle controls at 1 mg/kg.
Reduced the number of abdominal writhes by approximately 41% relative to vehicle controls at 5 mg/kg.
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Animal Model:C57BL/6J (male, 6 weeks old, 18-25 g, 49°C warm water-induced acute thermal pain model)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:i.p.; single dose
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Result:Increased tail-flick latency from a baseline of 3.92 s to 5.52 s at 1 h post-administration at 1 mg/kg.
Increased tail-flick latency from a baseline of 4.10 s to 6.14 s at 1 h post-administration at 5 mg/kg.
Produced a statistically significant increase in tail-flick latency relative to vehicle controls at 5 mg/kg.
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Animal Model:C57BL/6J (male, 6 weeks old, 18-25 g, formalin-induced mixed acute/inflammatory pain model)[1]
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Dosage:1 mg/kg; 5 mg/kg
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Administration:i.p.; single dose
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Result:Significantly reduced hind paw licking time during both Phase I and Phase II relative to vehicle controls at 1 mg/kg.
Produced a greater reduction in hind paw licking time during both Phase I and Phase II relative to vehicle controls at 5 mg/kg.
Yielded effects comparable to or greater than those of 10 mg/kg retigabine at 5 mg/kg.
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Animal Model:C57BL/6J (male, 6 weeks old, 18-25 g)[1]
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Dosage:1 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.p.; single dose
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Result:Did not significantly alter total travel distance relative to vehicle controls at all tested doses.
Did not significantly alter average movement speed relative to vehicle controls at all tested doses.
Did not significantly alter latency to fall from the rotarod relative to vehicle controls at all tested doses.
Chemical Information
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Peso molecular 363.42
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Fòrmula C23H22FNO2
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SMILES
CC1=CC(OCC2=CC=C(C=C2)F)=CC(C)=C1NC(CC3=CC=CC=C3)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fluoxakalner Related Classifications
HY-186240 Related Classifications
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