AAK1-IN-4
AAK1-IN-4 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 4.6 nM, Filt Ki of 0.9 nM, and cell IC50 of 8.6 nM). AAK1-IN-4 has the potential for the research for neuropathic pain.
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- No. CAS: 1815612-79-3
- Fòrmula: C20H28N4O3
- Peso molecular:372.46
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
In Vitro
AAK1-IN-4 (compound 43) (0.5 μM, 0-10 min) has good cell potencies of 2.4 in liver microsomes, as well as good metabolic stability (value of 95, 95, 93 for human, rat, and mouse microsomes, respectively) and no issue with CYP inhibitions[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AAK1-IN-4 (3 mg/kg; p.o; 0-7.5 hours) has good spinal cord penetration and spinal-cord-to-plasma-concentration ratios of 8.8[1].
AAK1-IN-4 (1-10 mg/kg; p.o.; 0-24.5 hours) can significantly reduces mechanical allodynia with over 80% peak inhibition of the pain response achieved at an oral dose of 10 mg/kg, and over 60% peak inhibition of the pain response at 3 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:Male Sprague-Dawley rats (chronic constriction injury, CCI)[1]
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Dosage:3 mg/kg
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Administration:p.o, 0-7.5 hours
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Result:Significantly reduced tactile allodynia with close to 80% inhibition of the pain response, as well as showed good spinal cord penetration and spinal-cord-to-plasma-concentration ratios of 8.8.
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Animal Model:Male Sprague-Dawley rats (STZ-induced diabetic peripheral neuropathic pain, DPNP) [1]
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Dosage:1-10 mg/kg
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Administration:p.o., 0-24.5 hours
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Result:Significantly reduced mechanical allodynia with over 80% peak inhibition of the pain response achieved at an oral dose of 10 mg/kg, and over 60% peak inhibition of the pain response at 3 mg/kg.
Chemical Information
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No. CAS 1815612-79-3
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Peso molecular 372.46
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Fòrmula C20H28N4O3
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SMILES
CC(C[C@](N)(COC1=CC=C(C2=CC=NC(NC(OC)=O)=C2)N=C1C)C)C
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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)
AAK1-IN-4 Related Classifications
HY-145838 Related Classifications
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