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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].

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $2,140 | 8-10 weeks | 8-10 weeks | |
| 50 mg | $2,785 | 8-10 weeks | 8-10 weeks | |
| 100 mg | $3,520 | 8-10 weeks | 8-10 weeks |
| Description | 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]. |
| In vitro | AAK1-IN-5 (compound 58), at a concentration of 0.5 μM administered over 0-10 minutes, demonstrates robust metabolic stability, exhibiting half-life durations exceeding 120 minutes in both human and mouse liver microsomes. In rat, cynomolgus monkey, and dog liver microsomes, its half-lives are recorded at 76.0, 17.6, and 26.0 minutes, respectively [1]. |
| In vivo | AAK1-IN-5 (compound 58) effectively reduces hyperalgesia in male Sprague-Dawley rats with chronic constriction injury (CCI) at dosages of 1 and 3 mg/kg. Administered orally within a 0-5.5 hour timeframe, this compound significantly alleviates pain symptoms associated with CCI, supporting its therapeutic potential in similar conditions [1]. |
| Molecular Weight | 385.4 |
| Formula | C19H23F4N3O |
| Cas No. | 1815613-44-5 |
| Smiles | C(F)(F)C=1C=C(N=CC1OC[C@@](CC(C)C)(C)N)C=2C=C(C(F)F)N=CC2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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