The cytosolic enzyme adenosine kinase (AK) catalyzes the transformation of adenosine into AMP. Adenosine kinase is one potential adenosine regulating agent (ARA) target. Because of its extremely brief plasma half-life (1 s), adenosine is primarily cleared through the activation of adenosine kinases. Increased intracellular adenosine produced as a result of adenosine kinase inhibition leaves the cell through passive diffusion or nucleoside transporters to activate adenosine receptors on nearby cell surfaces. Inhibiting adenosine kinase can therefore serve as a different mechanism for activating adenosine receptors and creating adenosine-related pharmacologies.
An alternative approach is to use adenosine kinase inhibitors (AKIs), which can increase local adenosine levels in a more site- and event-specific manner, elicit the desired pharmacology, and do so with a wider therapeutic window. In the rat maximal electric shock (MES) induced seizure assay, several potent AKIs are demonstrated to exhibit anticonvulsant activity.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V2588 | 5-Iodotubercidin (NSC-113939) | 24386-93-4 | 5-Iodotubercidin (also known as NSC 113939, 5-ITu)is a novel and potent adenosine kinase inhibitor with IC50 of 26 nM. |
|
V4402 | ABT-702 DIHYDROCHLORIDE | 1188890-28-9 | ABT-702 dihydrochloride is a novel and potentnon-nucleoside adenosine kinase(AK) inhibitor with IC50of 1.7 nM. |
|
V71235 | AK-IN-1 | 378775-98-5 | AK-IN-1 (compound 4072-2732) is an adenosine kinase (AK) inhibitor that is competitive for adenosine (Ado) but not ATP. |
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