| Chemical Properties | Back Directory | [form ]
Solid | [color ]
White to off-white | [Sequence]
H-{pY}-{AEEA}-Arg-Ser-Cys-Ile-Asp-Thr-Ile-Pro-Lys-Ser-Arg-Cys-Thr-Ala-Phe-Gln-Cys-Lys-His-Ser-Met-Lys-Tyr-Arg-Leu-Ser-Phe-Cys-Arg-Lys-Thr-Cys-Gly-Thr-Cys-NH2 (disulfide bridge:Cys5-Cys37,Cys14-Cys30,Cys19-Cys34) |
| Hazard Information | Back Directory | [Uses]
Dalazatide (ShK-186) is a specific Kv1.3 potassium channel peptide inhibitor. Dalazatide 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]. | [in vivo]
Dalazatide (ShK-186) (100 μg/kg; s.c.; once) inhibits delayed-type hypersensitivity and suppresses the in vivo motility and activation of Tem cells in rats[3]. | Animal Model: | Lewis rats rats, delayed-type hypersensitivity (DTH) model[3] | | Dosage: | 100 μg/kg | | Administration: | Subcutaneous injection, once | | Result: | Reduced DTH at all time points compared to rats given saline injections. Suppressed the proliferation of the Tem cells. |
| [References]
[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. DOI:10.1016/j.immuni.2008.07.015 |
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