Kv3 activator-1
Based on 1 Customer Validation
Kv3 activator-1 is a Kv3 family voltage-gated potassium channel activator. Kv3 activator-1 reverses mechanical hyperalgesia in rat models of neuropathic and inflammatory pain, with rapid onset and long-lasting, dose-related effects. Kv3 activator-1 can be used for the research of pain.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.41%
- No. CAS: 1380696-64-9
- Fòrmula: C20H20N4O4
- Peso molecular:380.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Actividad biológica
Descripciòn
In Vitro
Kv3 activator-1 (Compound X) increased whole-cell currents of Kv3.1 and Kv3.2 potassium channels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Kv3 activator-1 (10-60 mg/kg; i.p.; single dose) produces a dose-dependent reversal of mechanical hyperalgesia in a rat model of inflammatory pain, with peak efficacy of 92% reversal at the 60 mg/kg dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar Hanover (male, 225g, partial sciatic nerve ligation)[1]
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Dosage:10 mg/kg; 30 mg/kg; 60 mg/kg
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Administration:i.p.; single dose
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Result:Produced a dose-related reversal of mechanical sensitivity.
Reached peak reversal of 31% at 10 mg/kg, 73% at 30 mg/kg, and 81% at 60 mg/kg at 3 hours post-dose.
Increased contralateral paw withdrawal thresholds to mechanical pressure significantly.
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Animal Model:Wistar Hanover (male, 225g, intraplantar Freund's Complete Adjuvant (HY-153808) injection)[1]
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Dosage:10 mg/kg; 30 mg/kg; 60 mg/kg
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Administration:i.p.; single dose
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Result:Produced a dose-related reversal of mechanical sensitivity with rapid onset.
Reached peak reversal of 64% at 10 mg/kg at 3 hours post-dose, 74% at 30 mg/kg and 92% at 60 mg/kg at 1 hour post-dose.
Maintained significant reversal of 45% at 6 hours post-dose with 60 mg/kg.
Chemical Information
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No. CAS 1380696-64-9
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Appearance Solid
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Peso molecular 380.40
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Fòrmula C20H20N4O4
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Color White to light yellow
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SMILES
O=C1N(C2=CN=C(OC3=C4C5(CC5)COC4=C(C)C=C3)N=C2)C(C(C)(C)N1)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocolo
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Kv3 activator-1
- 1380696-64-9
- Potassium Channel
- Kv3.3 voltage-gated potassium channels
- Kv3 family voltage-gated potassium channel
- Kv3.1 voltage-gated potassium channels
- inflammatory pain
- whole-cell currents
- anti-hyperalgesic agent
- rat models
- Kv3.2 voltage-gated potassium channels
- mechanical hyperalgesia
- neuropathic pain
- Inhibitor
- inhibitor
- inhibit