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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C23H22FNO2
- Molecular Weight:363.42
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
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) |
In Vitro
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.
Parmacokinetics
In Vivo
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 (1-5 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) produces dose-dependent antinociceptive effects in a mouse model of CFA (HY-153808)-induced inflammatory pain[1].
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].
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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Molecular Weight 363.42
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Fluoxakalner Related Classifications
HY-186240 Related Classifications
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