1. Neuronal Signaling
  2. AAK1
  3. 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.

AAK1-IN-5 Chemical Structure

AAK1-IN-5 Chemical Structure

CAS No. : 1815613-44-5

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Description

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[1].

IC50 & Target

IC50: 1.2 nM (AAK1)[1].
Ki: 0.05 nM (AAK1)[1]

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

AAK1-IN-5 (compound 58) can reduce hyperalgesia in SD rats (chronic constriction injury) efficiently with good efficacy observed at doses of 1 and 3 mg/kg[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (chronic constriction injury, CCI)[1]
Dosage: 1-3 mg/kg
Administration: p.o., 0-5.5 hours
Result: Reduced hyperalgesia in CCI rats efficiently with good efficacy observed at doses of 1 and 3 mg/kg.
Molecular Weight

385.40

Formula

C19H23F4N3O

CAS No.
SMILES

CC(C[C@](N)(COC1=CN=C(C2=CC=NC(C(F)F)=C2)C=C1C(F)F)C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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AAK1-IN-5 Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AAK1-IN-5
Cat. No.:
HY-145839
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