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Kv1.3 channel distributes largely in immunocytes and in certain areas in the brain. Compelling evidence suggests its modulation of specified lymphocyte subsets, for example, activation and proliferation of autoreactive effector lymphocytes. Effector memory T cells contributes greatly to inflamed injuries in many autoimmune diseases such as multiple sclerosis, type-I diabetes, rheumatoid arthritis and transplant rejection. Inhibition of Kv1.3 can ameliorate autoimmune diseases in animal models. Selective Kv1.3 blockers, in particular, are more attractive for therapeutic use.
Kv1.3 has also been reported to regulate energy homeostasis and body weight suggesting that selective Kv1.3 blockers might have use in the management of obesity and insulin resistance.
In vitro electrophysiology Kv1.3 assay with manual patch clamp:
| Assay platform/method | Conventional patch clamp |
| Cells used in the assay | HEK293 Kv1.3 stable cell line |
| Measured parameters | Whole cell current of Kv1.3 channels |
| Test concentrations | 5 doses for IC50 |
| Data point repeats | N ≥ 3 for each concentration |
