ADWX 1 TFA is a novel peptide that potently targets and inhibits the Kv1.3 channel, with an IC50 of 1.89 pM. It specifically suppresses the activity of the Kv1.3 channel, in addition to inhibiting initial calcium signaling and NF-κB activation. This compound has been shown to ameliorate symptoms in rats with experimental autoimmune encephalomyelitis (EAE). ADWX 1 TFA is utilized in research focused on T-cell-mediated autoimmune diseases.

Kv1.1 channel:0.65nM(IC50), Kv1.3 channel:1.89pM(IC50)

ADWX 1 (1, 10 nM, 1 h) TFA selectively inhibits the activation of human CD4+ CCR7- T_EM cells by reducing levels of IL-2 and IFN-γ. Additionally, ADWX 1 (1, 10 nM, 50 min) TFA decreases [Ca2+] levels in activated CD4+ CCR7- T_CM cells derived from EAE rats. In a related effect, ADWX 1 (1, 10 nM, 1 h) TFA inhibits NF-κB activation in CD4+ CCR7- T cells activated by myelin basic protein (MBP) from EAE rats and specifically reduces levels of Kv1.3 gene and protein. Lastly, ADWX 1 (1, 10 nM, 3 days) TFA suppresses the activation of Th17 in CD4+ CCR7- T cells without inhibiting their differentiation.

ADWX 1 administered at 100 μg/kg/day via subcutaneous injection for three days effectively improved conditions in an experimental autoimmune encephalomyelitis (EAE) model in Sprague-Dawley rats by inhibiting the production of IL-2 and IFN-γ, and suppressing the proliferation of CCR7 - T_EM cells. Additionally, oral administration of ADWX 1 at doses of 5/10 mg/kg for two weeks did not induce any behavioral or pathological changes in the rats (acute toxicity study).