Dalazatide TFA  (Synonyms: ShK-186 TFA)

Dalazatide (ShK-186) TFA is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide TFA can be used in the study of autoimmune diseases such as multiple sclerosis (MS), lupus erythematosus, psoriasis, rheumatoid arthritis, type 1 diabetes and inflammatory bowel disease^[1][2][3].

Kv1.3^[1]

Dalazatide (ShK-186) (0-1000 pM) TFA 以剂量依赖的方式阻断卵巢特异性 GFP+ 效应记忆 T (Tem) 细胞中的 Kv1.3 电流，K_d 为 65 ± 5 pM^[3]。
Dalazatide (0-100 nM; 3 days) TFA 以剂量依赖的方式抑制 CCR7⁻ T 细胞增殖^[3]。
Dalazatide (100 nM; 30 min) TFA 通过抑制钙信号通路固定炎症部位的效应记忆 T (Tem) 细胞，从而阻止 β1 整合素激活^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Dalazatide (ShK-186) (100 μg/kg; s.c.; once) TFA 在大鼠中抑制延迟型超敏反应，并抑制 Tem 细胞的体内运动和激活^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

4442.08 (free acid)

C₁₈₄H₂₉₆N₅₇O₅₅PS₇._xC₂HF₃O₂

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Olsen C, et al. Dalazatide (ShK-186), a first-in-class peptide inhibitor of Kv1. 3 potassium channels, demonstrates safety, tolerability and proof of concept of efficacy in patients with active plaque psoriasis. J. Invest. Dermatol., 2016, 136(8).

  [2]. Stevens A M, et al. Thu0285 Dalazatide, an Inhibitor of the KV1. 3 Channel on Activated Effector Memory T Cells, Has Immunotherapy Potential in Systemic Lupus Erythematosus. 2016.

  [3]. Matheu MP, et al. Imaging of effector memory T cells during a delayed-type hypersensitivity reaction and suppression by Kv1.3 channel block. Immunity. 2008 Oct 17;29(4):602-14.  [Content Brief]