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.
性状
Solid
IC50 & Target[1][2]
Kv1.3
体外研究(In Vitro)
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,Kd 为 65 ± 5 pM。Dalazatide (0-100 nM; 3 days) TFA 以剂量依赖的方式抑制 CCR7 T 细胞增殖。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。 has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay-t
体内研究(In Vivo)
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。 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Lewis rats rats, delayed-type hypersensitivity (DTH)
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
Solvent&Solubility
In Vitro:
H2O
Peptide Solubility and Storage Guidelines:1. Calculate the length of the peptide.2. Calculate the overall charge of the entire peptide according to the following table:
参考文献
[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.