AAK1-IN-5
AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain.
For research use only. We do not sell to patients.
- CAS No.: 1815613-44-5
- Formula: C19H23F4N3O
- Molecular Weight:385.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
In Vitro
AAK1-IN-5 (compound 58) (0.5 μM, 0-10 min) has a good metabolic stability, with half-life values of over 120 min in human and mouse liver microsomes, and 76.0, 17.6, 26.0 min in rat, cynomolgus monkey, and dog, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
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:1-3 mg/kg
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Administration:p.o., 0-5.5 hours
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Result:Reduced hyperalgesia in CCI rats efficiently with good efficacy observed at doses of 1 and 3 mg/kg.
Chemical Information
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CAS No. 1815613-44-5
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Molecular Weight 385.40
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Formula C19H23F4N3O
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SMILES
CC(C[C@](N)(COC1=CN=C(C2=CC=NC(C(F)F)=C2)C=C1C(F)F)C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)