产品
编 号：F747293
分子式：C19H23F4N3O
分子量：385.4
分子式：C19H23F4N3O
分子量：385.4
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CAS No: 1815613-44-5
产品详情
生物活性：
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.
体内研究：
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.Animal Model:Male Sprague-Dawley rats (chronic constriction injury, CCI)
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.
体外研究：
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.
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.
体内研究：
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.Animal Model:Male Sprague-Dawley rats (chronic constriction injury, CCI)
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.
体外研究：
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.
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