HsTX1[R14A]

HsTX1[R14A] is a rationally engineered analogue of the scorpion toxin HsTX1, characterized as a **potent and selective peptide blocker of the voltage-gated potassium channel Kv1.3**. This 34-residue, C-terminally amidated peptide (derived from *Heterometrus spinnifer* venom), is stabilized by four disulfide bridges, increasing its stability in vivo[2][1]. The R14A mutation improves selectivity (>2,000-fold for Kv1.3 over Kv1.1) and maintains high affinity (IC50 ≈ 45 pM for Kv1.3)[2][1][4][5]. Selective inhibition of Kv1.3 suppresses the function and proliferation of CCR7− effector memory T cells and microglia, critical in mediating autoimmune and neuroinflammatory processes[4][5][6]. HsTX1[R14A] has demonstrated efficacy in animal models of rheumatoid arthritis, delayed-type hypersensitivity, and neuroinflammatory diseases, decreasing cytokine levels and inflammation[4][5][6][1]. The peptide is highly stable, shows good bioavailability, and can be administered intravenously, subcutaneously, or via pulmonary routes for systemic delivery[3][1][5].

Other names

HsTX1 mutant R14AHsTX-1 mutant R14AHsTX 1 mutant R14AKv1.3-blocking peptideKv-1.3-blocking peptideKv 1.3-blocking peptideHsTX1[R14Abu] (related but distinct analogue)