AAK1-IN-5

Name: AAK1-IN-5
Brand: TargetMol
SKU: T61693
Rating: 4.5 (1 reviews)

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产品编号 T61693Cas号 1815613-44-5

AAK1-IN-5 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), characterized by its ability to penetrate the central nervous system and its oral bioavailability. It displays high selectivity, with an AAK1 inhibitory potency (IC 50) of 1.2 nM, a binding affinity (K i) of 0.05 nM, and an inhibitory potency against cellular AAK1 activity (cell IC 50) of 0.5 nM. AAK1-IN-5 holds promise for investigating neuropathic pain in scientific research [1].

AAK1-IN-5

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产品编号 T61693Cas号 1815613-44-5

规格	价格	库存
25 mg	¥ 14,900	8-10周
50 mg	¥ 19,420	8-10周
100 mg	¥ 24,625	8-10周

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产品描述	AAK1-IN-5 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), characterized by its ability to penetrate the central nervous system and its oral bioavailability. It displays high selectivity, with an AAK1 inhibitory potency (IC 50) of 1.2 nM, a binding affinity (K i) of 0.05 nM, and an inhibitory potency against cellular AAK1 activity (cell IC 50) of 0.5 nM. AAK1-IN-5 holds promise for investigating neuropathic pain in scientific research [1].
体外活性	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].
体内活性	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]. 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.