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AAK1-IN-5
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Catalog No. T61693Cas No. 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
😃Good
Catalog No. T61693Cas No. 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].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 25 mg | $2,140 | 8-10 weeks | |
| 50 mg | $2,785 | 8-10 weeks | |
| 100 mg | $3,520 | 8-10 weeks |
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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