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AAK1-IN-4 

Cat. No.: HY-145838
Handling Instructions

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.

For research use only. We do not sell to patients.

AAK1-IN-4 Chemical Structure

AAK1-IN-4 Chemical Structure

CAS No. : 1815612-79-3

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Description

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[1].

IC50 & Target

IC50: 4.6 nM (AAK1)[1].
Ki: 0.9 nM (AAK1)[1]

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].

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; single) can significantly reduce tactile allodynia with close to 80% inhibition of the pain response in the rat CCI-induced pain model[1].
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].

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: 3 mg/kg
Administration: p.o, 0-7.5 hours
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.
Animal Model: Male Sprague-Dawley rats (STZ-induced diabetic peripheral neuropathic pain, DPNP) [1]
Dosage: 1-10 mg/kg
Administration: p.o., 0-24.5 hours
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.
Molecular Weight

372.46

Formula

C20H28N4O3

CAS No.
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Storage

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AAK1-IN-4
Cat. No.:
HY-145838
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