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Potent AAK1 inhibitor (IC50 values are 4.8 and 7.6 nM in enzyme and cell assays, respectively). Exhibits some selectivity for AAK1 over BIKE, and exhibits no significant activity at opioid, adrenergic α2 or GABAA receptors. Orally bioavailable. Peripherally restricted.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 410.47. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||4.87 mL||24.36 mL||48.72 mL|
|2.5 mM||0.97 mL||4.87 mL||9.74 mL|
|5 mM||0.49 mL||2.44 mL||4.87 mL|
|25 mM||0.1 mL||0.49 mL||0.97 mL|
References are publications that support the biological activity of the product.
Kostich et al (2016) Inhibition of AAK1 kinase as a novel therapeutic approach to treat neuropathic pain. J.Pharmacol.Exp.Ther. 358 371 PMID: 27411717
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